Category: 74572-29-5

Liu, Yongfu published the artcileDiscovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors, Recommanded Product: 5-Chloroisoindolin-1-one, the main research area is pyridyl isoindolinone derivative preparation oral aldosterone synthase inhibitor.

Aldosterone synthase (CYP11B2) inhibitors have been explored in recent years as an alternative therapeutic option to mineralocorticoid receptor (MR) antagonists to reduce elevated aldosterone levels, which are associated with deleterious effects on various organ systems including the heart, vasculature, kidney, and central nervous system (CNS). A benzamide pyridine hit derived from a focused screen was successfully developed into a series of potent and selective 3-pyridyl isoindolin-1-ones CYP11B2 inhibitors. Our systematic structure-activity relationship study enabled us to identify unique structural features that result in high selectivity against the closely homologous cortisol synthase (CYP11B1). We evaluated advanced lead mols., exemplified by compound 52, in an in vivo cynomolgus monkey acute adrenocorticotropic hormone (ACTH) challenge model and demonstrated a superior 100-fold in vivo selectivity against CYP11B1.

Journal of Medicinal Chemistry published new progress about Aldosterone synthase inhibitors. 74572-29-5 belongs to class indole-building-block, name is 5-Chloroisoindolin-1-one, and the molecular formula is C8H6ClNO, Recommanded Product: 5-Chloroisoindolin-1-one.

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

Ma, Rui-Jun published the artcileSynthesis of dihydro-[1,3]oxazino[4,3-a] isoindole and tetrahydroisoquinoline through Cu(OTf)2-catalyzed reactions of N-acyliminium ions with ynamides, Application of 5-Chloroisoindolin-1-one, the main research area is isoindole acetal ynamide copper catalyst cyclization; dihydrooxazinoisoindole preparation; tetrahydroisoquinoline acetal ynamide copper catalyst cyclization; dihydrooxazinoisoquinolinone preparation.

An efficient approach to access functionalized dihydro-[1,3]oxazino[4,3-a] isoindole and tetrahydroisoquinoline skeletons has been developed through the addition-cyclization process of ynamides with N-acyliminium ions generated from N,O-acetals. The reactions were conducted under the catalysis of Cu(OTf)2, and a number of functionalized dihydro-[1,3]oxazino[4,3-a] isoindoles and tetrahydroisoquinolines were generated in 48-98% yields. When chiral ynamides were used, optically pure tetrahydroisoquinolines could be obtained with good to excellent yields and diastereoselectivities.

Tetrahedron Letters published new progress about Acetals Role: RCT (Reactant), RACT (Reactant or Reagent). 74572-29-5 belongs to class indole-building-block, name is 5-Chloroisoindolin-1-one, and the molecular formula is C8H6ClNO, Application of 5-Chloroisoindolin-1-one.

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

Ma, Rui-Jun published the artcileSynthesis of 1-benzylisoindoline and 1-benzyl-tetrahydroisoquinoline through nucleophilic addition of organozinc reagents to N,O-acetals, Category: indole-building-block, the main research area is benzylisoindoline preparation; benzyl tetrahydroisoquinoline preparation; organozinc compound acetal nucleophilic addition.

A new approach to access 1-benzylisoindolines I [n = 1, 2; R1 = Bn, 4-FC6H4CH2, 4-t-BuC6H4CH2, etc.; R2 = H, 5-Br, 6-Cl, etc.] and 1-benzyl-tetrahydroisoquinolines I [R2 = H, 6,7-di-OMe] was developed through nucleophilic addition of organozinc reagents to N,O-acetals. A number of substituted organozinc reagents were amenable for this transformation, and the desired products were obtained with excellent yields. Moreover, Sc(OTf)3 proved to be an effective catalyst for the formation of 1-benzylisoindolines I and 1-benzyl-tetrahydroisoquinolines II using such nucleophilic addition

Organic & Biomolecular Chemistry published new progress about Isoindoles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 74572-29-5 belongs to class indole-building-block, name is 5-Chloroisoindolin-1-one, and the molecular formula is C8H6ClNO, 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

Zhang, Chunhui published the artcilePalladium-Catalyzed Direct C-H Carbonylation of Free Primary Benzylamines: A Synthesis of Benzolactams, Formula: C8H6ClNO, the main research area is primary benzylamine carbon monoxide carbonylation palladium; benzolactam preparation; palladium carbonylation.

A protocol for palladium-catalyzed C-H carbonylation of readily available free primary benzylamines using NH2 as the chelating group under an atm. pressure of CO has been achieved, providing a general, atom- and step-economic approach to benzolactams, an important structural motif found in many biol. active compounds Application of this new method is also exemplified in the concise syntheses of two bioactive mols, e.g., (R)-PD 172939.

Organic Letters published new progress about Aralkyl amines Role: RCT (Reactant), RACT (Reactant or Reagent) (primary). 74572-29-5 belongs to class indole-building-block, name is 5-Chloroisoindolin-1-one, and the molecular formula is C8H6ClNO, Formula: C8H6ClNO.

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