BMS 201038-04

한글명:BMS 201038-04

카스 번호202914-84-9

상품명:BMS 201038-04

CBNumberCB02627605

분자식C40H41F6N3O5S

포뮬러 무게789.8260592

MOL 파일202914-84-9.mol

화학적 성질

저장 조건	Inert atmosphere,Room Temperature
용해도	DMSO:100.0(Max Conc. mg/mL);126.61(Max Conc. mM) Ethanol:100.0(Max Conc. mg/mL);126.61(Max Conc. mM)
물리적 상태	Solid
색상	White to off-white
CAS 데이터베이스	202914-84-9

그림문자(GHS)

BMS 201038-04 화학적 특성, 용도, 생산

개요
Lomitapide is an orally active microsomal triglyceride transfer protein (MTP) inhibitor for the treatment of hypercholesterolemia. The drug was developed by Aegerion Pharmaceuticals Inc. and licensed to Bristol–Myers Squibb Co. and the University of Pennsylvania. Lomitapide effectively lowered LDL–cholesterol, both as a single agent and in combination with commonly prescribed lipid-lowering therapies. Sold under the trade name Juxtapid, the drug offers a new treatment option to patients who cannot tolerate statin therapy or who experience insufficient LDL–cholesterol reduction with the currently available therapies, such as patients with homozygous familial hypercholesterolemia caused by mutations in the LDLR gene.
정의
ChEBI: A methanesulfonate (mesylate) salt prepared from equimolar amounts of lomitapide and methanesulfonic acid. Used as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.
Synthesis
Commercial 9H-fluorene-9-carboxylic acid (105) was alkylated with 1,4-dibromobutane in the presence of n-butyl lithium in THF to give 9-(4-bromobutyl)-9H-fluorene-9-carboxylic acid (106) in 85% yield. Next, activation of the acid as the acid chloride followed by coupling with (2,2,2-trifluoroethylamine) provided amide 107 in 71% yield for the two-step sequence. Displacement of the terminal bromide with the appropriate 4-carbamoyl piperidine followed by removal of the Boc group furnished piperidinyl fluorine 108 in high yield. Amine 108 was then reacted with the acid chloride derived from acid 109 (derived from the Suzuki coupling of boronic acid 110 and o-iodobenzoic acid 111) to give lomitapide, and this was followed by salt formation with methanesulfonic acid to afford lomitapide mesylate (XIV).

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