TOFOGLIFLOZIN

TOFOGLIFLOZIN 속성

TOFOGLIFLOZIN C화학적 특성, 용도, 생산

개요

Tofogliflozin hydrate, which is a sodium-glucose co-transporter 2 inhibitor, was approved in Japan for the treatment of type 2 diabetes at the same time as luseogliflozin hydrate (XIX). The drug was discovered by Chugai Pharmaceutical and jointly developed with Sanofi-Aventis and Kowa. Tofogliflozin hydrate reduces glucose levels by inhibiting the reuptake of glucose by selectively inhibiting SGLT2, and plays a key role in the reuptake of glucose in the proximal tubule of the kidneys.

Synthesis

Reduction of commercially available 2-bromoterephtalic acid (268) through the use of trimethoxyborane and borane- THF proceeded in 89% yield to afford diol 269. Subjection of this compound to 2-methoxypropene (270) under acidic conditions generated bis-acetonide 271. This bromide then underwent lithium¨Chalogen exchange followed by exposure to magnesium bromide and treatment with lactone 272 (which was prepared by persilylation of commercially available (3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2Hpyran- 2-one (277). This mixture was worked up with aqueous ammonium chloride and upon treatment with p-TsOH in methanol resulted in spiroacetal 273. Next, global protection of all alcohol functionalities within 273 was affected by reaction with methylchloroformate and DMAP in acetonitrile. The benzyl carbonate within 274 was selectively exchanged via Suzuki coupling with 4-ethylphenylboronic acid (275) to afford methylene dibenzyl system 276. Subsequent treatment with aqueous sodium hydroxide in methanol followed by crystallization from 1:6 acetone and water furnished the desired product tofogliflozin hydrate (XXXIV) in 75% yield.

TOFOGLIFLOZIN 준비 용품 및 원자재

원자재

준비 용품

TOFOGLIFLOZIN 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Anqing Chico Pharmaceutical Co., Ltd.	15380796838	chloewu@chicopharm.cn	CHINA	340	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22963	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
career henan chemical co	+86-0371-86658258 +8613203830695	factory@coreychem.com	China	29809	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32161	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
Qiuxian Baitai New Material Co., LTD	+8618330912755	sale2@hbyalin.com	China	1658	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-89586680 +86-18192503167	1026@dideu.com	China	7724	58
AFINE CHEMICALS LIMITED	+86-0571-85134551	sales@afinechem.com	China	15352	58
Henan Alfa Chemical Co., Ltd			China	12341	58

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