专利号:EP-1735276-B1 优先权日:2004-04-02 标题:Novel method for the preparation of intermediates useful for the synthesis of vitamin d analogues 发明人:HANSEN ERIK TORNGAARD; SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; PEDERSEN HENRIK; DEUSSEN HEINZ-JOSEF WILHELM 权利人:LEO PHARMA AS 摘要:The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
专利号:US-2016073631-A1 优先权日:2013-03-04 标 题 :Process for the preparation of dihydropyrrole derivatives 发明人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS 权利人:SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) n n n n n n n n n n n n wherein n P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; n R 1 is chlorodifluoromethyl or trifluoromethyl; n R 2 is optionally substituted aryl or optionally substituted heteroaryl; n n is 0 or 1; n including the process comprising n (a-i) reacting a compound of formula II n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; n with nitromethane in the presence a chiral catalyst to give a compound of formula III n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; and n (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. n n n n n The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
专利号:WO-2014138989-A1 优先权日:2013-03-15 标 题 :Method and intermediates for the synthesis of hydroxamic acid compounds 发明人:VAISBURG ARKADII; RAEPPEL FRANCK; ROY SIMON; ZHOU NANCY Z 权利人:METHYLGENE INC 摘要:Methods are disclosed for making a compound of formula and intermediates therefor, where R is aryl or heteroaryl, and L is C3_8alkylene, wherein each of R, L, and the illustrated phenyl group are independently optionally substituted with one or more substituents selected from the group consisting of C].6alkyl, Ci.6alkoxy, CF3, CHF2, CH2F, fluoro, and cyano, which methods can avoid the use of iodo-phenyl esters, or aryl alkynes, or both, or, in which synthetic methods at least one of the intermediates is a solid at room temperature that does not require purification by chromatography.
专利号:US-9233920-B2 优先权日:2010-06-11 标题 :Process for the preparation of dihydropyrrole derivatives 发明人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS 权利人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS; SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R 1 is chlorodifluoromethyl or trifluoromethyl; R 2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R 1 and R 2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R 1 and R 2 are as defined for the compound of formula I; and (a-ii) reductively cyclizing the compound of formula III to give the compound of formula I. The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
专利号:US-2009131660-A1 优先权日:2006-04-03 标 题 :SYNTHESIS OF 3-[4-(1,1-DIMETHYL-PROPYL)-PHENYL]-2-METHYL-PROPIONALDEHYDE AND cis-4--2,6-DIMETHYL-MORPHOLINE (AMOROLFINE) 发明人:BOITEAU JEAN-GUY; MUSICKI BRANISLAV 权利人:GALDERMA SA 摘要:3-[4-(1,1-Dimethyl-propyl)-phenyl]-2-methyl-propionaldehyde and cis-4-{3-[4-(1,1-dimethyl-propyl)-phenyl]-2-methyl-propyl}-2,6-dimethyl-morpholine (Amorolfine) are synthesized, first by Heck reacting a compound of general formula (VI): n n n n n n n n n n with 2-methyl-prop-2-en-1-ol of formula (VII): n n n n n n n n n n in the presence of a palladium catalyst and a base, in a solvent selected from among N,N-dimethylformamide, polar protic and non-polar organic solvents, and at a temperature ranging from 60° C. to 150° C., and then conducting an amino reduction by reacting the 3-[4-(1,1-dimethyl-propyl)-phenyl]-2-methyl-propionaldehyde of formula (II) with cis-2,6-dimethyl morpholine of formula (IV): n n n n n n n n n n in the presence of a reducing agent and in a solvent.
参考文献:10.1107/s1600536811017764 摘要:Wang H, Xia G, Liu X, Shen J. (2R,6S)-tert-Butyl 2-(benzhydrylcarbamoyl)-6-methylmorpholine-4-carboxylate. Acta Crystallogr E Struct Rep Online. 2011 May 20;67(6):o1437. doi: 10.1107/s1600536811017764. 参考文献:10.1371/journal.pone.0021403 摘要:Limpert E, Stahel WA. Problems with Using the Normal Distribution – and Ways to Improve Quality and Efficiency of Data Analysis. PLoS ONE. 2011 Jul 14;6(7):e21403. doi: 10.1371/journal.pone.0021403.