Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于三氯化磷体系中,化学反应生成氯乙基异氰酸酯 参考文献:Syntheses From Ethanolamine. Iii. Synthesis Of N-β-Chloroethyl Urethan And Of β-Chloroethyl Isocyanate 标题:Syntheses From Ethanolamine. Iii. Synthesis Of N-β-Chloroethyl Urethan And Of β-Chloroethyl Isocyanate 摘要: Doi:10.1021/ja01303A065
专利号:US-2023192601-A1 优先权日:2020-05-11 标 题:Scaled-up synthesis of lomustine under control flow conditions 发明人:THOMPSON DAVID HARLEY; Nagy Zoltan Kalman; MUFTI AHMED; MACKEY JARON 权利人:PURDUE RESEARCH FOUNDATION 摘要:The present disclosure provides processes and apparatuses for the scaled-up manufacture of lomustine via continuous flow manufacture. Such continuous flow processes may optionally include the crystallization of lomustine and the apparatuses may optionally include crystallization apparatuses/reactors in either batch or continuous flow design. In one aspect of the disclosure, a process for making lomustine is provided comprising treating solutions of 2-chloroethylisocyanate with a solution of cyclohexylamine with continuous-flow pumps in a gram-flow reactor to form a combined solution, adding deionized water with a continuous flow-pump to the combined solution to form a liquid-organic phase solution, extracting the organic phase from the solution and treating with a solution of t-butyl nitrite with a continuous flow pump in a gram flow reactor to form lomustine.
专利号:US-10941111-B2 优先权日:2018-10-16 标 题:On-demand rapid synthesis of lomustine under continuous flow conditions 发明人:THOMPSON DAVID H; COOKS ROBERT GRAHAM; FERREIRA CHRISTINA RAMIRES; JAMAN ZINIA 权利人:PURDUE RESEARCH FOUNDATION 摘要:Disclosed herein is a continuous manufacturing process for lomustine that has a short residence time and 63 percent yield. Major advantages of this process are that the total production cost for lomustine is lower, the product is higher quality, and the manufacturing operation is safer for production personnel.
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-9265773-B2 优先权日:2011-09-08 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI; MERCK SHARP & DOHME; MSD ITALIA SRL 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:WO-2024061972-A1 优先权日:2022-09-20 标 题:Methods and platform for chemical synthesis 发明人:CRONIN LEE; MANZANO SEBASTIÃ?N; ZALESSKIY SERGEY; KITSON PHILIP; WANG HSIN 权利人:UNIV GLASGOW COURT 摘要:The invention relates to a method and apparatus for performing and characterising a chemical synthesis, such as those performed with an automated chemical synthesis platform, including such that are portable platforms, the method comprising the steps of: performing a chemical synthesis in a chemical synthesiser; recording analytical data during the chemical synthesis, and developing a profile for the analytical data recorded over time; and comparing the profile for the chemical synthesis against a reference profile, which reference profile is the analytical data recorded over time for a reference chemical synthesis, wherein the chemical synthesis and the reference chemical synthesis share at least the same reagents and method steps for the same intended product, such as the chemical synthesis and the reference chemical synthesis sharing the same instruction set. The method and apparatus are for intended for use in replication of approved, chemical syntheses based on common reaction platforms.
专利号:US-5777076-A 优先权日:1994-10-24 标题 :Method for peptide synthesis starting from N- (N'-nitrosocarbamoyl) amino acids 发明人:COMMEYRAS AUGUSTE; COLLET HELENE; MION LOUIS; BENEFICE SYLVIE; CALAS PATRICK; CHOUKROUN HENRI; TAILLADES JACQUES; BIED CATHERINE 权利人:UNIV MONTPELLIER II 摘要:A method for peptide synthesis using an N- N'-nitroso-(R')carbamoyl!amino acid as the starting compound. The compound is separated into N 2 , R'OH and N-carboxyanhydride of formula (II). ##STR1## The compound (II) together with an amino acid or peptide with at least one free α-amino function is introduced into a reactive medium to obtain a dipeptide or a higher peptide than the added peptide.
摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2019) 1, 397. 参考文献:10.1007/bf00422493 摘要:Lijinsky W, Taylor HW. Carcinogenicity of chlorinated nitrosotrialkylureas in rats. Journal of Cancer Research and Clinical Oncology. 1979 Jan;94(2):131–7. doi: 10.1007/bf00422493. 参考文献:10.1021/jm200488a 摘要:Fortin S, Wei L, Moreau E, Lacroix J, Côté MF, Petitclerc E, Kotra LP, C-Gaudreault R. Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4. J Med Chem. 2011 Jul 14;54(13):4559–80. 参考文献:10.1007/s00280-003-0740-7 摘要:Penketh PG, Shyam K, Baumann RP, Remack JS, Brent TP, Sartorelli AC. 1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[(methylamino)carbonyl]hydrazine (VNP40101M): I. Direct inhibition of O6-alkylguanine-DNA alkyltransferase (AGT) by electrophilic species generated by decomposition. Cancer Chemother Pharmacol. 2004 Apr;53(4):279–87. doi: 10.1007/s00280-003-0740-7.