专利号:WO-2024201393-A1 优先权日:2023-03-29 标 题:Methods for the synthesis of nucleoside analogues and nucleosides analogues derived therefrom 发明人:BRITTON ROBERT; Muir Garrett; ANKETELL MATTHEW JAMES; HUXLEY COHAN; BAIKABI SUPING 权利人:UNIV FRASER SIMON 摘要:The present invention relates to methods for the synthesis of nucleoside analogues. More specifically, the present invention relates to methods for the synthesis of C4' substituted nucleoside analogues via the reaction of a soft nucleophile with a halohydrin ketone.
专利号:US-11198684-B2 优先权日:2017-07-28 标 题 :Intermediates useful for the synthesis of a selective inhibitor against protein kinase and processes for preparing the same 发明人:OH SANG-HO; KHOO JA-HEOUK; LIM JONG-CHUL; LEE DOO-BYUNG; LEE JUNG-AE; LEE JUN-SUP; JU HYUN; SHIN WOO-SEOB; JEON SANG-SEOL 权利人:YUHAN CORP 摘要:The present invention provides intermediates useful for the synthesis of an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors; and processes for preparing the same. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.
专利号:US-5304647-A 优先权日:1988-02-09 标题:Method of preparation of halogenated diazines 发明人:STREKOWSKI LUCJAN; MOKROSZ MARIA; HARDEN DONALD B 权利人:UNIV GEORGIA STATE 摘要:A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof. The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product. The substituted halogenodiazines are used as intermediates in the synthesis of unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.
专利号:US-2006009642-A1 优先权日:2001-10-12 标题 :Methods for the synthesis of substituted purines 发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G 权利人:IRM LLC 摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.
专利号:US-6143748-A 优先权日:1995-03-31 标题:Process for synthesis of nucleoside analogues 发明人:SAMANO MIRNA C; SAMANO VICENTE; GOODYEAR MICHAEL DAVID 权利人:GLAXO WELLCOME INC 摘要:The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the β-diastereomer, and intermediates useful in the process.
专利号:US-8242273-B2 优先权日:2005-07-28 标 题:Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine 发明人:DENG XIAOHU; MANI NEELAKANDHA 权利人:DENG XIAOHU; MANI NEELAKANDHA; JANSSEN PHARMACEUTICA NV 摘要:This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the corresponding 1,2-diketones, and cyclocondensation reactions.
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合成参考文献
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