专利号:US-5541347-A 优先权日:1993-12-07 标 题 :Synthesis of bisindolylmaleimides 发明人:FAUL MARGARET M; JIROUSEK MICHAEL R; WINNEROSKI II LEONARD L 权利人:LILLY CO ELI 摘要:The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
专利号:US-6239313-B1 优先权日:2000-02-16 标 题 :Process for the solid state synthesis of enantiopure B-aminoalcohols from racemic epoxides 发明人:KAKULAPATI RAMA RAO; NANDURI BHANUMATHI; ELETI RAJENDER REDDY 权利人:COUNCIL SCIENT IND RES 摘要:The invention relates to a process for the solid state synthesis of enantiopure β-aminoalcohols by preparing inclusion complexes of aryloxyepoxide with cyclodextrin by adding an epoxide in equimolar ratio in an organic solvent to an aqueous solution of cyclodextrin, reacting the cyclodextrin complex of aryloxyepoxide with a nucleophile in solid state by intimately grinding the mixture using a mortar and pestle, continuing the mixing till the starting epoxide disappeared on tic, removing excess amines under vacuum, extracting the β-aminoalcohols produced with a solvent with yields of more than 50% and enantioselectivity of upto 100%.
专利号:US-5591852-A 优先权日:1990-08-10 标题 :Process for the preparation of nucleotides 发明人:VEMISHETTI PURUSHOTHAM; BRODFUEHRER PAUL R; HOWELL HENRY G; SAPINO JR CHESTER 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:The present invention relates to a novel and economical process for the synthesis of HPMP-substituted nucleotide antiviral compounds. Also disclosed are novel intermediates produced in the process for the preparation of HPMPC.
专利号:US-5714597-A 优先权日:1994-07-07 标题:Use of carbocation scavenger during oligonucleotide synthesis 发明人:RAVIKUMAR VASULINGA; ANDRADE MARK; MULVEY DENNIS; COLE DOUGLAS L 权利人:ISIS PHARMACEUTICALS INC 摘要:During the synthesis of oligonucleotides and phosphate linked oligomers, a carbocation scavenging agent is employed to increase the overall yield. The carbocation scavenging agent is used in conjunction with an acidic solution employed during the deprotection step.
专利号:US-2005043376-A1 优先权日:1996-12-03 标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A 摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.
专利号:US-8431714-B2 优先权日:2007-04-16 标题:Synthesis of drug conjugates via reaction with epoxide-containing linkers 发明人:MCKENNA CHARLES E; KASHEMIROV BORIS A; BALA JOY LYNN F 权利人:MCKENNA CHARLES E; KASHEMIROV BORIS A; BALA JOY LYNN F; UNIV SOUTHERN CALIFORNIA 摘要:The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.
摘要:Stankevič, M.; Pietrusiewicz, K. M., Science of Synthesis Knowledge Updates, (2013) 2, 339. 摘要:Matsumoto, K.; Katsuki, T.; Arends, I. W. C. E., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 70. 摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 147. 摘要:Wever, R.; Babich, L.; Hartog, A. F., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 243. 摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 161.