专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:WO-2025082632-A1 优先权日:2023-10-16 标 题:Method and composition for oligonucleotide synthesis 发明人:SAITO MASAHARU 权利人:BACHEM HOLDING AG 摘要:The invention pertains to a method for the synthesis of oligonucleotides using pseudo solid-phase protecting groups, wherein said method comprises a step of subjecting a solution comprising a component (C-0)# to one or more aqueous extractions, wherein the organic phase comprises the component (C-0)#. Said component (C-0)# is a nucleoside or an oligonucleotide, which is covalently bonded to a pseudo solid-phase protecting group and comprises a free backbone hydroxyl group. The aqueous phase of each of said one or more aqueous extractions has a pH-value in the range of 4-7.
专利号:EP-4605403-A1 优先权日:2022-10-17 标 题:Method and composition for oligonucleotide synthesis 发明人:SAITO MASAHARU; TAKEDA KAZUTAKA; OKADA YOHEI; LUTHER ANATOL 权利人:BACHEM HOLDING AG 摘要:The invention pertains to methods for the synthesis of oligonucleotides using pseudo solid-phase protecting groups, wherein said method comprises at least one aqueous extraction carried out in the presence of one or more amide solvents SA, wherein each amide solvent SA is an amide solvent comprising one or more alkyl groups, wherein these one or more alkyl groups together comprise in total 6−24 carbon atoms. The invention further pertains to compositions comprising an oligonucleotide which is covalently bonded to a pseudo solid-phase protecting group and a mixed solvent comprising on or more of the aforementioned amide solvents SA.
专利号:WO-2024083746-A1 优先权日:2022-10-17 标 题 :Method and composition for oligonucleotide synthesis 发明人:SAITO MASAHARU; TAKEDA KAZUTAKA; OKADA YOHEI; LUTHER ANATOL 权利人:BACHEM HOLDING AG 摘要:The invention pertains to methods for the synthesis of oligonucleotides using pseudo solid-phase protecting groups, wherein said method comprises at least one aqueous extraction carried out in the presence of one or more amide solvents SA, wherein each amide solvent SA is an amide solvent comprising one or more alkyl groups, wherein these one or more alkyl groups together comprise in total 6−24 carbon atoms. The invention further pertains to compositions comprising an oligonucleotide which is covalently bonded to a pseudo solid-phase protecting group and a mixed solvent comprising on or more of the aforementioned amide solvents SA.
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: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).
[参考文献]: K Yoneto, Et Al. Influence Of The Permeation Enhancers 1-Alkyl-2-Pyrrolidones On Permeant Partitioning Into The Stratum Corneum. J Pharm Sci. 1998 Feb;87(2):209-14.
合成参考文献
摘要:United States Environmental Protection Agency, Office of Pesticides and Toxic Substances., 8EHQ-1290-1125 摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 352.