On November 10, 2016, Lan, Jiong; Zhou, Fusheng; Zhao, Jinzhu; Xu, Feng; Shi, Xia; Xie, Jing; Xu, Hui; Wang, Lixiao published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Bicyclic substituted benzene sulfonamide derivatives as voltage-gated sodium channel inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:
The invention relates to bicyclic substituted benzene sulfonamide derivatives of formula I, and the preparation method and pharmaceutical use as voltage-gated sodium channel inhibitors in the treatment of diseases thereof. In particular, disclosed in the present invention are the compounds of formula I or their pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof, and the preparation method and use thereof. Compounds of formula I wherein R1-R4 are independently H, OH, CN, NO2, halo, NH2 and derivatives, C1-20 alkyl, C3-20 cycloalkly, etc.; R5 is 5- to 6-membered heteroaryl, -CO-C1-20 alkyl, C3-20 cycloalkyl; L1 and L2 are independently a bond, -(CH2)1-3, etc.; dotted double bond is either a single bond or a double bond; X is a bond, NH and derivatives, O, S; Z1 is (un)substituted CH2, O, -CO-, (un)substituted -CH=, -N=, etc.; Z2 is -CO-, (un)substituted CH2, -NH- and derivatives, =N-, (un)substituted =CH-, O, etc.; Z3 is NH and derivatives, CH2, (un)substituted -CH=, etc.; Z4 is a bond, NH and derivatives, CH2, (un)substituted =CH-, =N-, etc.; ring A is (un)substituted 5- to 6-membered (hetero)aryl, etc.; and their pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs as voltage-gated sodium channel inhibitors useful in the treatment of diseases thereof, are claimed. Compounds of formula I were prepared by using condensation as the key step. All the invention compounds were evaluated for their voltage-gated sodium channel inhibitory activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole
The Article related to benzenesulfonamide preparation voltage gated sodium channel inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 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