专利号:US-9174943-B2 优先权日:2010-02-24 标 题 :Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds 发明人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT 权利人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT; MEDIVATION PROSTATE THERAPEUTICS INC 摘要:Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
专利号:WO-2019199375-A1 优先权日:2018-04-10 标 题 :Synthesis of boron complexes with oxygen-containing multidentate ligands 发明人:LU GANG 权利人:DOW SILICONES CORP 摘要:A method for preparing a boron complex is provided. The method comprises contacting and allowing to react at a temperature from 0 to 100°C: (a) an alkoxyborane of formula (I) wherein R1 and R2 independently are hydrogen, C1-C30 hydrocarbyl or C5-C30 heterocyclic; and R3 is C1-C30 hydrocarbyl; and (b) either (i) an α-diketo compound having from 4 to 30 carbon atoms, or (ii) a β-diketo compound having from 5 to 50 carbon atoms. A method for addition reaction polymerization using the boron complex obtained by said method is also provided.
专利号:US-2017190670-A1 优先权日:2014-07-11 标题:Improved process for the preparation of enzalutamide 发明人:HIRPARA SANJAY; SHRAWAT VIMAL KUMAR; POTHURAJU RAJU; TRIPATHI CHANDRESH KUMAR; AKSHAYKANT CHATURVEDI 权利人:SHILPA MEDICARE LTD 摘要:The present application relates to an improved process for preparation of Enzalutamide (I). n n n n n n n n n n The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. n The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.
专利号:US-9045462-B2 优先权日:2012-08-17 标 题 :Synthesis of an antiviral compound 发明人:EVANS JARED WAYNE; FUJIMORI SHINJI; HUYNH GRACE M; LIU QI; TERESK MARTIN GERALD 权利人:GILEAD SCIENCES INC 摘要:The present disclosure provides processes for the preparation of a compound of Formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
专利号:US-8927741-B2 优先权日:2012-08-17 标 题 :Synthesis of an antiviral compound 发明人:WATKINS WILLIAM JOHN; LIU QI 权利人:GILEAD SCIENCES INC 摘要:The present disclosure provides a processes for the preparation of a compound of Formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of Formula I.
专利号:US-6255475-B1 优先权日:1995-01-31 标 题:Chain terminators, the use thereof for nucleic acid sequencing and synthesis and a method of their preparation 发明人:KWIATKOWSKI MAREK 摘要:The invention relates to compounds of general structure (I) or salts thereof, wherein B is a nucleobase, X and Z independently are oxygen or sulphur, Y is hydrogen or hydroxy, which optionally may be protected, R 1 is hydrocarbyl, which optionally is substituted with a functional group, R 2 is hydrogen or hydrocarbyl, which optionally is substituted with a functional group, A is an electron withdrawing or electron donating group capable of moderating the acetal stability of compound (I), L 1 and L 2 are hydrocarbon linkers, which may be the same or different, L 2 , when present, being either (i) connected to L 1 via the group A, or (ii) directly connected to L 1 , the group A then being connected to one of linkers L 1 and L 2 , F is a dye label, Q is a coupling group for F, and l, m and n independently are 0 or 1, with the proviso that l is 1 when m is 1, and l is 1 and m is 1 when n is 1. The compounds of formula (I) are useful as deactivatable chain extension terminators. The invention also relates to the use of the compounds (I) in nucleic acid synthesis and nucleic acid sequencing as well as to a method of preparing compounds of Formula (I).
[参考文献]: Cédric Bouteiller, Et Al. Copper-Catalyzed Amination Of (Bromophenyl)Ethanolamine For A Concise Synthesis Of Aniline-Containing Analogues Of Nmda Nr2B Antagonist Ifenprodil. Org Biomol Chem. 2010 Mar 7;8(5):1111-20. [参考文献]: Emilia Iglesias, Et Al. Tautomerization Of 2-Acetylcyclohexanone. 1. Characterization Of Keto-Enol/enolate Equilibria And Reaction Rates In Water. J Org Chem. 2003 Apr 4;68(7):2680-8. [参考文献]: Zhiyu Jia, Et Al. An Alternative To The Classical α-Arylation: The Transfer Of An Intact 2-Iodoaryl From Ari(Occf). Angew Chem Int Ed Engl. 2014 Oct 13;53(42):11298-301.
合成参考文献
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