On October 28, 2010, Kawano, Tomoaki; Yonetoku, Yasuhiro; Hanazawa, Takeshi; Nigawara, Takahiro; Fukudome, Hiroki; Moritani, Hiroshi published a patent.Category: indole-building-block The title of the patent was Preparation of diacylethylenediamine compounds as DGAT1 inhibitors. And the patent contained the following:
Title compounds I [A = (un)substituted aryl, (un)substituted cycloalkyl, (un)substituted heteroaryl, etc.; ring B1 = phenylene, pyridinediyl, naphthalenediyl, etc. (herein phenylene, pyridinediyl and naphthalenediyl are optionally substituted with hydroxy, alkyl, halo, etc.); W = -O-, bond, -NH-, etc.; ring B2 = cyclohexanediyl, cyclopentanediyl or bridged ring (herein cyclohexanediyl, cyclopentanediyl and bridged ring are optionally substituted with alkyl); Y = bond, alkylene or -O-alkylene; Z = -CO2H [or biol. equivalent group thereof], carbamoyl (optionally substituted with Ph or benzyl), -OH, etc.] or salts thereof were prepared For example, reaction of Et trans-4-hydroxycyclohexanecarboxylate with benzyl 4-hydroxybenzoate in the presence of 1,1′-(azodicarbonyl)dipiperidine followed by debenzylation, EDCI-mediated amidation with tert-Bu (2-aminoethyl)carbamate, treatment with HCl, carbamoylation with trans-2-phenylcyclopropyl isocyanate, and hydrolysis afforded compound II [R = trans-2-phenylcyclopropylamino; X = H]. In diacylglycerol acyltransferase 1 (DGAT1) inhibition assays, compound II [R = 5-fluorobenzothien-2-yl; X = F] showed IC50 of 0.1 nM. Compounds I are claimed useful for the treatment of obesity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Category: indole-building-block
The Article related to diacylethylenediamine preparation dgat1 inhibitor, obesity treatment diacylethylenediamine dgat1 inhibition, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters 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