📜劳森试剂 以 苯 用作溶剂,以27 Mg (50%)的收率获得噻二唑 参考文献:Novel Photoactivable Fluorescent Dyes For Optical Microscopy And Imaging Techniques 标题:Novel Photoactivable Fluorescent Dyes For Optical Microscopy And Imaging Techniques 摘要:本发明涉及以下通式g1-G4(i)的新型光致发色基础或羧基吡咯烷衍生物,其中:G1:A1=o,A2=n,A3=c;G2:A1=s,A2=n,A3=c;G3:A1=o,A2=o,A3=n;G4:A1=s,A2=o,A3=n;包括吸收紫外光的色团,经过254-490 Nm的光解作用(最好在375-420 Nm下),产生荧光的罗丹明或羧基吡咯烷衍生物和小的无毒碎片,例如n2或n2O.本发明还涉及制备这种化合物的方法以及将这些化合物用于光学显微镜和成像技术的使用.
专利信息
专利号:US-10711138-B2 优先权日:2016-04-08 标题:Intermediates and procedures for the synthesis of functional materials 发明人:KIRSCH PEER; GUNST SUSANN 权利人:MERCK PATENT GMBH 摘要:The present invention relates to heteroaromatic compounds which have two different reactive groups, their use in the synthesis of asymmetrically substituted compounds, and synthesis processes in which the compounds according to the invention are reacted sequentially with two different compounds, whereby an asymmetrically substituted compound is formed.
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-11459549-B2 优先权日:2018-05-10 标 题:Method for biocatalytic synthesis of Sitagliptin and intermediate thereof 发明人:WU FAHAO; YANG WEN; LI GANG; SHI HONGWEI; GAO YANGZHE; LIU LILI; YUAN ZHIFA 权利人:CHINA FORTUNE WAY COMPANY; NANJING REDWOOD FINE CHEMICAL CO LTD 摘要:Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.
专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-6096898-A 优先权日:1999-10-22 标 题:One pot synthesis of 1,2,4-triazoles 发明人:PODHOREZ DAVID E; HULL JR JOHN W; BRADY CHRISTINE H 权利人:DOW AGROSCIENCES LLC 摘要:One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.
专利号:US-7423171-B2 优先权日:2006-06-20 标题 :One-step catalytic process for the synthesis of isocyanates 发明人:SERRANO FERNANDEZ FRANCISCO LU; ALMENA MUNOZ BEATRIZ; PADILLA POLO ANA; OREJON ALVAREZ ARANCHA; CLAVER CABRERO CARMEN; CASTILLON MIRANDA SERGIO; SALAGRE CARNERO PILAR; AGHMIZ ALI 权利人:REPSOL YPF SA 摘要:A one-pot process for the synthesis of isocyanates, polyisocyanates or mixtures thereof which includes the steps of:n i. preparing a mixture comprising an amine, an alcohol, an oxygen-containing gas, carbon monoxide, a metal complex catalyst selected from the group consisting of macrocyclic complex catalysts and cobalt Shiff base catalysts; and a solvent selected from the group consisting of aliphatic or aromatic halocarbons, perhalogenated alcohols, halogenated ethers, halogenated ketones, perfluorinated hydrocarbons, polymers of chlorotrifluoroethylene having the formula —(CF 2 —CFCl) n wherein n is between 2 and 10, and mixtures thereof; ii. subjecting the resulting mixture to a first heating under pressure; iii. cooling and depressurizing the mixture resulting from the previous step; and iv. subjecting the mixture of the previous step to a second heating to separate out the isocyanate product from the mixture.
参考文献:10.1107/s1600536811011391 摘要:Tahir MN, Khan MU, Hammed S, Bokhari TH, Hina S. 6-(1-Adamant-yl)-3-(2-chloro-phen-yl)-1,2,4-triazolo[3,4-b][1,3,4]thia-diazole. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1022. 参考文献:10.1107/s1600536811007343 摘要:Banu A, Begum NS, Lamani RS, Khazi IM. 6-(4-Bromo-phen-yl)-2-(4-fluoro-benz-yl)imidazo[2,1-b][1,3,4]thia-diazole. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o779. 参考文献:10.1107/s1600536811007665 摘要:Mo Q, Duan W, Ma X, Huang J, Ma Z. 2-Chloro-N-{5-[(4R,5R,10S)-dehydroabiet-4-yl]-1,3,4-thiadiazol-2-yl}benzamide. Acta Crystallogr E Struct Rep Online. 2011 Mar 09;67(4):o816–7. doi: 10.1107/s1600536811007665. 参考文献:10.1107/s1600536811008841 摘要:Yu P, Wang P, Zhang JQ, He Q, Wan R. (E)-N-(4-Chloro-benzyl-idene)-5-(4-methyl-phen-yl)-1,3,4-thia-diazol-2-amine. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o861. 参考文献:10.1107/s1600536811017107 摘要:Zhi S, Mu S, Liu Y, Liu D. N-(5-Ethylsulfanyl-1,3,4-thiadiazol-2-yl)-2-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-5-yl)acetamide. Acta Crystallogr E Struct Rep Online. 2011 May 25;67(6):o1490. doi: 10.1107/s1600536811017107.