Recently I am researching about OPTIMIZING POTENCY; NA(V)1.7; SULFONAMIDES; PHARMACOKINETICS; DISCOVERY; CHANNELS; TARGETS, Saw an article supported by the . Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Stumpf, A; Cheng, ZK; Beaudry, D; Angelaud, R; Gosselin, F. The CAS is 100-51-6. Through research, I have a further understanding and discovery of Benzyl Alcohol. Product Details of 100-51-6
The development of a redesigned and improved second-generation synthesis of the Nav1.7 inhibitor GDC-0276 based on experience gained from a fit-for-purpose first-generation synthesis will be described. The first-generation synthesis proceeded via a regioselective SNAr reaction on the advanced starting material t-butyl 5-chloro-2,4-difluorobenzoate with 1-adamantanemethanol. In the newly developed second-generation synthesis, the much improved regioselective SNAr reaction was performed on the readily available starting material 1-chloro-2,4-difluorobenzene, followed by installation of the carboxylate group by electrophilic aromatic bromination and a palladium-catalyzed alkoxycarbonylation. A subsequent Suzuki-Miyaura cross-coupling reaction was then telescoped directly into a phase-transfer-catalyzed ester hydrolysis. Amidation of the resulting acid intermediate with 1-azetidine sulfamide in turn provided GDC-0276 in high overall yield and purity on a 100 kg scale.
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Reference:
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