N-Benzyl N-(Tert-Butoxycarbonyl) Toluenesulfonamide置于palladium Dihydroxide 氢气体系中,用 乙醇 用作溶剂,以96%的收率获得n-(叔丁氧羰基)对甲苯磺酰胺 参考文献:A Reversible Safety-Catch Method For The Hydrogenolysis Of N-Benzyl Moieties 标题:A Reversible Safety-Catch Method For The Hydrogenolysis Of N-Benzyl Moieties 摘要:The Benzyl Groups Of Beta-Hydroxy-N-Benzyl Sulfonamides Are Labile Toward Hydrogenolysis-Unlike N-Benzyl Sulfonamides Lacking The Beta-Hydroxy Moiety. We Find That N-Acyl-N-Benzyl Sulfonamides Undergo Hydrogenolysis Under Very Mild Conditions. Based Upon These Observations,We Developed A Reversible Safety-Catch Method Using Tert-Butoxycarbonyl Moieties To Activate N-Benzyl Sulfonamides Toward Hydrogenolysis. We Also Explored The Utility Of The Safety-Catch Activation Method For Other Nitrogen-Based Functionality Such As N-Benzyl Carboxamides,Imides,And Related Functionality. (C) 2004 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tetlet.2004.09.118
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-RE41614-E 优先权日:1998-09-30 标题 :Synthetic analogs of ecteinascidin-743 发明人:COREY ELIAS J 权利人:HARVARD COLLEGE 摘要:The present invention is directed to the synthesis and characterization of compounds having the formula: n n wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO 2 R′, NO 2 , NH 2 , NHR′, N(R′) 2 , NHC(â•?O)R′ NHC( â•?O ) R′ , CN, halogen, â•?O, C(â•?O)H, C(â•?O)R′, CO 2 H, CO 2 R′, C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH 2 , NO 2 , SH, CN, halogen, â•?O, C(â•?O)H, C(â•?O)CH 3 , CO 2 H, CO 2 CH 3 , C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R 7 and R 8 may be are joined into a carbocyclic or heterocyclic ring system; and wherein X 1 and X 2 are each independently defined as above for R 1 -R 8 R 1 - R 6 and R 9 , an each further includes specific preferred groups as defined herein.
专利号:WO-2013065066-A1 优先权日:2011-11-02 标 题 :Processes for preparing 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [l,2,41-triazolo[43-a]pyrazin-7(8h)-yl]-l-(2,4,5- trifluorophenyl)butan-2-amine 发明人:PANDEY BIPIN; DAVE MAYANK GHANSHYAMBHAI; KOTHARI HIMANSHU M; SHUKLA BHAVIN SHRIPRASAD; MENDIRATTA SANJEEV KUMAR; JOSHI RUPAL; TRIVEDI UMANG 权利人:CADILA HEALTHCARE LTD; PANDEY BIPIN; DAVE MAYANK GHANSHYAMBHAI; KOTHARI HIMANSHU M; SHUKLA BHAVIN SHRIPRASAD; MENDIRATTA SANJEEV KUMAR; JOSHI RUPAL; TRIVEDI UMANG 摘要:The present invention relates to synthesis of 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [l,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2- amine of Formula (I) either in its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms by novel processes. The invention further relates to certain novel intermediates useful in the preparation of compound of Formula (I) and processes for their preparation.
专利号:CN-114539304-B 优先权日:2022-02-18 标题:Synthesis method and application of a class of 1,3-azasilane compounds