202914-84-9 Usage
Description
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.
Definition
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).
Check Digit Verification of cas no
The CAS Registry Mumber 202914-84-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,0,2,9,1 and 4 respectively; the second part has 2 digits, 8 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 202914-84:
(8*2)+(7*0)+(6*2)+(5*9)+(4*1)+(3*4)+(2*8)+(1*4)=109
109 % 10 = 9
So 202914-84-9 is a valid CAS Registry Number.
202914-84-9Relevant articles and documents
CRYSTALLINE POLYMORPH OF N-(2,2,2-TRIFLUOROETHYL-9-[4-[R4-R[[[I4'- (TRIFLUOROMETHYL) [ 1,1 ' -BIPHENYL] -2-YL] CARBONYL] AMINO] -1 -PIPERIDINYL] BUTYL] -9H- FLUORENE-9-CARBOXAMIDE METHANESULFONATE AND PROCESS FOR PREPARATION THEREOF
-
, (2017/07/06)
The present invention relates to? crystalline polymorph of N-(2,2.2-trifluoroethyl)-9- [4- [4- [ [[4,-(trifluoromethyl) [1,1 '-biphenyl] -2-yl] carbonyl] amino] - 1 -piperidinyl] butyl] -9H- fluorene-9-carboxamide methanesulfonate salt represented by the following structural formula- la and process for preparation thereof.
AMORPHOUS FORM OF LOMITAPIDE MESYLATE
-
, (2016/05/02)
Provided is novel amorphous form of lomitapide mesylate salt and process for preparation thereof.
Crystal form III of lomitapide mesylate
-
Paragraph 0048; 0049; 0050, (2016/12/01)
The invention provides a crystal form III of lomitapide mesylate. An X-ray diffraction pattern of the crystal form comprises diffraction peaks obtained when a diffraction angle 2theta is equal to 9.912 degrees, 11.584 degrees, 14.651 degrees, 15.444 degre
