474645-92-6Relevant academic research and scientific papers
SYNTHESIS OF IMIDE COMPOUNDS
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Page/Page column 11-13; 17-18, (2008/12/05)
The invention relates to a process for the production of an imide (1) (2) (3) via the enantioselective addition of an amine (2) to an alkene (3) wherein Y is OR, wherein R is alkyl or Bn, said process comprising: incubating Pd(OTf)2 with a phos
A concise asymmetric synthesis of torcetrapib
Guino, Meritxell,Pim, Huat Phua,Caille, Jean-Claude,King, Kuok Hii
, p. 6290 - 6293 (2008/02/10)
(Chemical Equation Presented) Optically active torcetrapib was synthesized in seven steps from achiral precursors without the need for protecting groups, utilizing an enantioselective aza-Michael reaction to achieve asymmetry.
Asymmetric synthesis of the cholesteryl ester transfer protein inhibitor torcetrapib
Damon, David B.,Dugger, Robert W.,Hubbs, Stephen E.,Scott, Jill M.,Scott, Robert W.
, p. 472 - 480 (2012/12/22)
Previously our group reported synthetic efforts used to synthesize kilogram quantities of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, 1, via a mid-stage resolution. This account describes research conducted to develop an asymmetri
PROCESS FOR PRODUCING OPTICALLY ACTIIVE BETA-AMINO ACID DERIVATIVES
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Page/Page column 52-53, (2010/02/10)
The present invention is to provide a method for producing the desired optically active β-amino acid derivatives of high optical purities in high yields, without requiring a step of deprotection. More particularly, the present invention relates to a metho
METHOD FOR PRODUCING AN OPTICALLY ACTIVE TETRAHYDROQUINOLINE
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Page 77, (2008/06/13)
The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a β-ketoester of formula (2) with an amine of formula (3) to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active β-amino acid derivative of formula (5); 3) a step of amidating the optically active β-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).
Method for producing (R) -3- [4- (trifluoromethyl) phenylamino] -pentanoic acid amide derivative
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Page 18, (2010/02/08)
The present invention provides a method for easily producing an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative useful for an intermediate for pharmaceutical products, particularly an inhibitor of a cholesteryl ester transfer protei
