Day: November 4, 2022

On March 10, 2005, Chang, Hye-Kyung; Oh, Yeong-Koo; Park, Cheol-Won; Jang, Yong-Jin; Park, Tae-Kyo; Kim, Sung-Sub; Kim, Min-Jung; Park, Mi-Jeong; Park, Jung-Gyu; Park, Hee-Dong; Min, Kyeong-sik; Lee, Tae-soo; Lee, Sang-kyun; Kim, Soo-hyeon; Jeong, Hee-kyung; Lee, Sun-hwa; Kim, Hwa-dong; Kim, Ae-ri; Park, Ki-sook; Shin, Hyun-ik; Choi, Hyeong-wook; Lee, Kyu-woong; Lee, Jae-hoon; Heo, Tae-ho; Kim, Ho-jun; Kwon, Tae-sik published a patent.HPLC of Formula: 883526-76-9 The title of the patent was Preparation of carbamoylisoxazoles as caspase inhibitors. And the patent contained the following:

Isoxazoles I [R = H, alkyl, cycloalkyl, aryl, aralkyl; R1 = alkyl, cycloalkyl, aryl, aralkyl, amino acid residue; R2 = alkyl, cycloalkyl, aryl, aralkyl, amino acid residue, H, substituted hydroxyalkyl; A = bond, O alkylene, oxaalkylene, (un)substituted NH2; B = H, alkyl, cycloalkyl, aralkyl; CRR1 = carbocyclic or heterocyclic ring; X = acyl, substituted CH:CHCOH, CH:CHSO2H] were prepared for use as caspase inhibitors in the prevention of inflammation and apoptosis. Thus, PhCCl:NOH was treated with CH2:CEtCO2Et ti give Et 5-ethyl-3-phenyl-4,5-dihydro-5-isoxazolecarboxylate (II). Tert.-Bu (3S)-3-amino-4-hydroxy-5-(2,3,5,6-tetrafluorophenoxy)pentanoate (III) was prepared from 2,3,5,6-F4CHOH and N-benzyloxycarbonyl-L-aspartic acid β-tert.-Bu ester. Amidation of III with II and deblocking gave the title compound IV which had Ki for caspase inhibition of 1.9 M-1 min-1. The experimental process involved the reaction of 1,5-Dimethyl-1H-indole-2-carbaldehyde(cas: 883526-76-9).HPLC of Formula: 883526-76-9

The Article related to carbamoylisoxazole preparation caspase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.HPLC of Formula: 883526-76-9

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 10, 2000, Gwaltney, Stephen L., II; Jae, Hwan-Soo; Kalvin, Douglas M.; Liu, Gang; Sham, Hing L.; Li, Qun; Claiborne, Akiyo K.; Wang, Le; Barr, Kenneth J.; Woods, Keith W. published a patent.Safety of 6-Chloro-1H-indole-5-carboxylic acid The title of the patent was Preparation of substituted oxazolines as antiproliferative agents. And the patent contained the following:

The title compounds [I; R1-R3 = alkyl, alkoxy, thioalkoxy; R4, R5 = H, alkyl; R6 = (un)substituted aryl, heterocyclyl, cycloalkyl, etc.], useful for treating cancer, were prepared E.g., a multi-step synthesis of I [R1-R3 = 3,4,5-(MeO)3; R4, R5 = H; R6 = 4-Me2NC6H4] which showed 100% inhibition in both 48-h cellular proliferation assays that used human colon adenocarcinoma, MDR pos. and human lung cell carcinoma, MDR neg., was given. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Safety of 6-Chloro-1H-indole-5-carboxylic acid

The Article related to oxazoline preparation antiproliferative antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Safety of 6-Chloro-1H-indole-5-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Cai, Xianrong; Wang, Chao; Sun, Jian published an article in 2012, the title of the article was Organocatalytic Enantioselective Dipolar [3+2] Cycloadditions of Acetylenic Aldehydes with Nitrones for the Formation of Chiral 4-Isoxazolines.Name: H-Idc-OH And the article contains the following content:

An organocatalytic enantioselective protocol has been developed for the dipolar [3+2] cycloaddition between acetylenic aldehydes and nitrones through an iminium activation pathway. This protocol uses L-α,α-bis(3,5-ditrifluoromethylphenyl)prolinol as catalyst and 3,5-dinitrobenzoic acid as additive and is friendly for one-pot operation for the nitrone formation and the subsequent cycloaddition It also exhibits a broad substrate scope and allows for the highly efficient production of chiral 4-isoxazolines with various substituents under mild conditions in high yields (68-92%) with high enantioselectivities (up to 96% ee). The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Name: H-Idc-OH

The Article related to isoxazoline stereoselective preparation alkynal aldehyde nitrone prolinol catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Name: H-Idc-OH

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On May 8, 2001, Gwaltney, Stephen L., II; Jae, Hwan-Soo; Kalvin, Douglas M.; Liu, Gang; Sham, Hing L.; Li, Qun; Claiborne, Akiyo K.; Wang, Le; Barr, Kenneth J.; Woods, Keith W. published a patent.HPLC of Formula: 256935-86-1 The title of the patent was Preparation of oxazoline antiproliferative agents. And the patent contained the following:

R2ZR [I; R = alkyl-, alkoxy, or alkylthio-trisubstituted Ph; R2 = (un)substituted cycloalk(en)yl, -heterocyclyl, -aryl, etc.; Z = (4-alkyl)-2-oxazoline-2,5-diyl or 4,4-dialkyl-2-oxazoline-2,5-diyl] were prepared Thus, 3,4,5-trimethoxybenzaldehyde was condensed with MeNO2 and the reduced product amidated by 4-(Me2N)C6H4COCl to give, after cyclization, I [R = C6H2(OMe)3-3,4,5, R2 = C6H4(NMe2)-4, Z = 2-oxazoline-2,5-diyl]. Data for biol. activity of I were given. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to oxazoline preparation antiproliferative agent, antitumor agent oxazoline preparation, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.HPLC of Formula: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On November 1, 2014, Yang, Jun; Zhou, Shanshan; Ji, Liyan; Zhang, Chao; Yu, Siwang; Li, Zhongjun; Meng, Xiangbao published an article.Name: 6-Chloro-2,3-dihydro-1H-indole The title of the article was Synthesis and structure-activity relationship of 4-azaheterocycle benzenesulfonamide derivatives as new microtubule-targeting agents. And the article contained the following:

A series of 1-sulfonyl indolines was synthesized and evaluated for antiproliferative activity. The most potent compounds I (R = H or MeO) showed significant cytotoxicity (IC50 in the range of 0.055-0.105 and 0.039-0.112 μM, resp.) against four human cancer cell lines HCT116, PC3, HepG2 and SK-OV-3. The structure-activity relationship of this series of sulfonamides, including the influence of azaheterocycle rings, substituent at the different positions of indolines, and the cyclopropane moiety, was described. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Name: 6-Chloro-2,3-dihydro-1H-indole

The Article related to indoline azaheterocycle benzenesulfonamide preparation microtubule targeting agent antitumor, benzenesulfonamides, indoline, microtubule-targeting agents, synthesis, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Name: 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On April 30, 1980, Kaneko, Chikara; Fujii, Harue; Kawai, Shinji; Yamamoto, Atsushi; Hashiba, Kazuhiko; Kimata, Toshihiko; Hayashi, Reiko; Somei, Masanori published an article.Application In Synthesis of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Studies on the N-oxides of π-deficient N-heteroaromatics. XXXIV. Studies on oxazepine derivatives. X. A novel synthesis of substituted indoles by photochemical ring contraction of 3,1-benzoxazepines. And the article contained the following:

A novel photochem. ring-contraction reaction of 3,1-benzoxazepines I (R = cyano, Ph; R1 = Cl, CO2H; R2 = H) yields 3-formylindoles II (R3 = CHO, R4 = H, Cl) in an aprotic solvent. This ring contraction was successfully extended to oxazepines having an alkoxycarbonyl function at the 5-position to give the indoles having this function at the 3-position. Though most of the oxazepines underwent the ring-contraction reaction only on irradiation at 254 nm, 5-carboxy derivatives or their esters afforded the ring-contraction products even at ≥300 nm. The intermediacy of 3H-indole species in these photochem. ring-contraction reactions was demonstrated by the isolation of II (R = Ph, R3 = Ac, R4 = 5-CO2Me) during the photolysis of I (R = Ph, R1 = COOMe, R2 = Me) this 3H-indole afforded II (R = Ph, R3 = Ac, R4 = 4-, and 6-CO2Me) upon further irradiation The mechanism of this acetyl migration is discussed based on the result of the photochem. acetyl migration of Me 1-acetyl-2-phenylindole-3-carboxylate. The oxazepines were obtained by photochem. rearrangement of quinoline oxides at ≥300 nm. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Application In Synthesis of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to benzoxazepine ring contraction photochem, indole preparation photochem, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Application In Synthesis of Methyl 2-methyl-1H-indole-3-carboxylate

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On December 16, 2015, Liu, Zhaotie; Liu, Huan; Wang, Chao; Chen, Jiangang; Liu, Zhongwen; Xiao, Jianliang published a patent.Synthetic Route of 52537-00-5 The title of the patent was A recyclable supported cyclic metal iridium catalyst and its preparation method and application in dehydrogenation reaction of indoline series compound. And the patent contained the following:

The present invention discloses a recyclable supported cyclic metal iridium catalyst and its preparation method and application in dehydrogenation reaction of indoline series compound The catalyst is pyrene-labeled cyclic metal iridium complex, which uses multi-walled carbon nanotubes as carrier. The pyrene-labeled cyclic metal iridium complex has structural formula as in Claim 1. The cyclic metal iridium complex uses iridium atom as coordination center, uses 4-methoxy-N-[1-(4- hydroxyphenyl)methylene]-aniline and pentamethyl cyclopentadiene as ligand. The preparation method includes: synthesis of 4-methoxy-N-(1-(4-hydroxyphenyl)methylene)-aniline; (2) synthesis of cyclic metal iridium complex; (3) synthesis of pyrene-labeled cyclic metal iridium complex; (5) preparation of the supported cyclic metal iridium catalyst. The inventive catalyst has simple preparation method, short preparation period, can achieve dehydrogenation reaction of indoline series compound in green solvent (mixed solvent of water and trifluoroethanol); the reaction conditions are mild, safe, green and efficient. The inventive catalyst can be recycled through simple centrifuge separation, and can keep its excellent catalytic performance after reused many times. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Synthetic Route of 52537-00-5

The Article related to recyclable supported cyclic metal iridium catalyst dehydrogenation indoline, Catalysis, Reaction Kinetics, and Inorganic Reaction Mechanisms: Catalysts and other aspects.Synthetic Route of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 2, 2020, Ma, Dawei; Ji, Yuhua; He, Weiming; Fang, Chao; Zhao, Jinlong; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Li, Ying published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 3, 2020, Ma, Dawei; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Zhao, Jinlong; Li, Ying published a patent.Category: indole-building-block The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Category: indole-building-block

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On November 25, 2015, Meng, Xiangbao; Yang, Jun; Li, Zhongjun published a patent.Recommanded Product: 52537-00-5 The title of the patent was Preparation of 4-substituted benzene sulfonamide derivative and their application as anticancer agents. And the patent contained the following:

The invention is related to the preparation of 4-substituted benzene sulfonamide derivative and their application as anticancer agents. The invention compounds I, wherein R1 is H, halogen, etc.; R2-R5 are independently selected from H, nitro, cyano, etc.; X is -C(R6R7)-, carbonyl, O, etc.; Y is -C(R6R7)-, O, or -N(R8)-; Z is O or S; W is N or CH; M is C1-4 linear or branched alkyl or cyclopropyl; R6 R7 and R8 are each independently selected from H, C1-4 alkyl; and their pharmaceutically acceptable salts, solvates are claimed. Compound I was prepared by multi-step procedure (procedure given). The invention compounds were evaluated for their anticancer activity. From assay, it was determined that I exhibited the IC50 value of 0.029-1.187 uM against HCT116. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 52537-00-5

The Article related to preparation substituted benzene sulfonamide derivative application anticancer agents, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Recommanded Product: 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles