专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2004249170-A1 优先权日:2002-01-24 标 题 :Process for preparing an intermediate useful for the asymmetric synthesis of duloxetine 发明人:BORGHESE ALFIO 摘要:This invention provides a process for the synthesis of(S)-3-Methylamino-1-2-thienyl)-1-propanol, a key intermediate in the synthesis of duloxetine.
专利号:US-5491243-A 优先权日:1993-10-12 标题 :Intermediate useful for the asymmetric synthesis of duloxetine 发明人:BERGLUND RICHARD A 权利人:LILLY CO ELI 摘要:This invention provides a stereospecific process for the synthesis of (S)-(+)-N,N-dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine, a key intermediate in the synthesis of duloxetine.
专利号:US-8367868-B2 优先权日:2006-10-16 标题:Process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine 发明人:BERTOLINI GIORGIO; VERZOLA BARBARA; VERGANI DOMENICO 权利人:ARCHIMICA SRL; BERTOLINI GIORGIO; VERZOLA BARBARA; VERGANI DOMENICO 摘要:The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: n nwhere: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-7538232-B2 优先权日:2006-01-19 标 题 :Process for the asymmetric synthesis of duloxetine 发明人:BUTCHKO MARK ANTHONY; MERSCHAERT ALAIN; MODER KENNETH PHILIP 权利人:LILLY CO ELI 摘要:This invention provides an improved asymmetric process for the synthesis of duloxetine involving arylation of Compounds of Formula I.
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