151851-75-1Relevant articles and documents
PRODUCTION METHOD OF (R)-2-AMINO-2-ETHYLHEXANOL
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Paragraph 0130, (2017/01/02)
PROBLEM TO BE SOLVED: To easily and efficiently produce (R)-2-amino-2-ethylhexanol that is useful as a pharmaceutical intermediate without carrying out a complicated operation. SOLUTION: (R)-2-amino-2-ethylhexanol is produced by subjecting a N-benzylidene-2-amino ester derivative to asymmetric alkylation by using an optically active phase transfer catalyst and subsequently subjecting the derivative to removal of benzylidene, reduction and the like. Further the obtained product is made to react with an optically active acid to form a salt to precipitate a solid product. Thus, a solid of the (R)-2-amino-2-ethylhexanol salt is obtained to improve optical purity. COPYRIGHT: (C)2015,JPOandINPIT
Hypolipidemic 1,4-benzothiazepine derivative
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Page 15, (2010/01/31)
The invention is concerned with a novel hypolipidemic compound, which is of (3R,5R)-3-Butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-5-phenyl-1,4-benzothiazepin-8-ol 1,1-dioxide; or a salt, solvate, or physiologically functional derivative thereof, with processes for its preparation, pharmaceutical compositions containing it and with its use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as athersclerosis.
Hypolipidaemic condensed 1,4-thiazepines
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, (2008/06/13)
The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R1 is hydrogen or C1-6 alkyl; R2 is an atom or group selected from hydrogen, C1-4 alkyl (including cycloalkyl and cycloalkylalkyl), C1-4 alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R3 is hydrogen, OH, C1-6 alkyl, C1-6 alkoxy or --O C1-6 acyl; R4 is a group independently selected from C1-6 alkyl (including cycloalkyl and cycloalkylalkyl), C2-6 alkenyl, and C2-6 -alkynyl which groups are optionally substituted; R5 is a group independently selected from C2-6 alkyl (including cycloalkyl and cycloalkylalkyl), C2-6 alkenyl and C2-6 alkynyl, which groups are optionally substituted; or R4 and R5, together with the carbon atom to which they are attached, form a C3-7 spiro cycloalkyl group which is optionally substituted; R6 and R7 are independently selected from hydrogen and C1-6 alkyl; and X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur, or X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic compounds. STR1
