专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-8461357-B2 优先权日:2008-09-19 标题 :Expeditious synthesis of gibberellin A5 and esters thereof 发明人:FAIRWEATHER KELLY A; MANDER LEWIS N; PHARIS RICHARD P 权利人:FAIRWEATHER KELLY A; MANDER LEWIS N; PHARIS R P; UTI LIMITED PARTNERSHIP 摘要:An expeditious synthesis of gibberellin A 5 (GA 5 ) esters is presented, from which GA 5 may be prepared. The synthesis offers an inexpensive route of few steps to these compounds, starting from gibberellin A 3 (GA 3 ) esters in the presence of a metal hydride.
专利号:US-2010069644-A1 优先权日:2008-09-15 标题:Method of regio-selective synthesis of tri-substituted-1, 2, 3-triazoles 发明人:SHI XIAODONG 权利人:SHI XIAODONG 摘要:The embodiments provide for region-selective synthesis of tri-substituted 1,2,3-traizoles. A first embodiment provides for the selective N-2 alkylation of a 4,5-disubstituted 1,2,3-triazole. A second embodiment provides for the selective acetylation of a 4,5-disubstituted 1,2,3-triazole. A third embodiment provides for the selective arylation of a 4,5-disubstituted 1,2,3-triazole.
专利号:WO-2024137329-A1 优先权日:2022-12-20 标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
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-4912253-A 优先权日:1988-06-06 标题 :Method for the preparation of an unsaturated alcohol or ester thereof 发明人:FUKUMOTO TAKEHIKO; YAMAMOTO AKIRA 权利人:SHINETSU CHEMICAL CO 摘要:An efficient method is proposed for the synthesis of an unsaturated alcohol of the general formula R--CHâ•?CH(CH 2 ) n+1 OH, in which R is a hydrogen atom or a monovalent hydrocarbon group having 1 to 10 carbon atoms and the subscript n is an integer in the range from 3 to 10, in which an acetate of the formula R--CHâ•?CHCH 2 OCOCH 3 is subjected to a coupling reaction with a Grignard reagent of the formula X 1 Mg(CH 2 ) n OMgX 2 , in which X 1 and X 2 are each a halogen atom, and then the reaction product is hydrolyzed. When the reaction product of the coupling reaction is reacted with acetic anhydride instead of hydrolysis, the corresponding acetate can readily be obtained. These unsaturated alcohols and acetates form a class of important biologically active compounds or intermediates thereof including sex pheromone compounds of insects.
摘要:Collings, J. C., Science of Synthesis Knowledge Updates, (2013) 4, 220. 摘要:Muñiz, K., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 10. 摘要:Kirschning, A.; Gille, F.; Wolling, M., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 1, 426. 摘要:Martínez, C.; Muñiz, K., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 309.