202914-84-9

Basic information

• Product Name: BMS 201038-04
• Synonyms: BMS 201038-04;LoMitapide Mesylate;BMS 201038 methanesulfonic acid salt;AEGR 733 Mesylate;AEGR733 Mesylate;AEGR-733 Mesylate;BMS 201038 Mesylate;BMS201038 Mesylate
• CAS NO: 202914-84-9
• Molecular Formula: C40H41F6N3O5S
• Molecular Weight: 789.8260592
• Product Categories: Inhibitors
• Mol File: 202914-84-9.mol

Chemical Properties

• Appearance: /
• Storage Temp.: Inert atmosphere,Room Temperature
• CAS DataBase Reference: BMS 201038-04(CAS DataBase Reference)
• NIST Chemistry Reference: BMS 201038-04(202914-84-9)
• EPA Substance Registry System: BMS 201038-04(202914-84-9)

Safety Data

• Hazardous Substances Data: 202914-84-9(Hazardous Substances Data)

Usage

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).

Upstream product

• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 182438-98-8 9-(4-bromo-butyl)-9H-fluorene-9-carboxylic acid-(2,2,2-trifluoro-ethyl)-amide 
• 180340-74-3 4'-trifluoromethylbiphenyl-2-carbonyl chloride 
• 331767-53-4 9-(4-bromo-butyl)-9H-fluorene-9-carboxylic acid chloride 
• 182438-97-7 9-(4-bromo-butyl)-9H-fluorene-9-carboxylic acid 
• 128796-39-4 4-trifluoromethylphenylboronic acid 
• 88-67-5 2-Iodobenzoic acid 
• 182439-41-4 N-(1-piperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide 
• 50541-93-0 4-amino-1-benzylpiperidine 
• 84392-17-6 4'-(trifluoromethyl)-2-biphenylcarboxylic acid 
• 3002-30-0 methyl 9H-fluorene-9-carboxylate 
• 1989-33-9 9H-fluorene-9-carboxylic acid 

Relevant 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

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.

PROCESS FOR THE PREPARATION OF LOMITAPIDE

The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.

AMORPHOUS FORM OF LOMITAPIDE MESYLATE

Provided is novel amorphous form of lomitapide mesylate salt and process for preparation thereof.

PROCESS FOR MAKING LOMITAPIDE MESYLATE

The present disclosure provides a process for lomitapide and its pharmaceutically acceptable salts. The present disclosure further provides pharmaceutically acceptable salts (e.g., 5 mesylate) of lomitapide in amorphous form.

Crystal form III of lomitapide mesylate

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

New crystal forms of lomitapide mesylate and preparation method thereof

The invention provides a new crystal form I and a new crystal form II of lomitapide mesylate and a preparation method thereof. An X-ray diffraction diagram of the crystallization form of the crystal form I contains diffraction peaks at the diffraction ang

POLYMORPHIC FORMS OF LOMITAPIDE AND ITS SALTS AND PROCESSES FOR THEIR PREPARATION

The present invention relates to various polymorphic forms of lomitapide or its salts and processes for preparation thereof. The present invention provides Lomitapide mesylate in solid amorphous form and process for preparation thereof. The invention also