专利号:US-11976081-B2 优先权日:2019-04-26 标题 :Intermediate of eribulin and synthesis method and use thereof 发明人:XU WEIPING 权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD 摘要:An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.
专利号:WO-2014128524-A1 优先权日:2013-02-19 标题:An improved process for preparation of an intermediate of the pyrrolidine substituted flavones 发明人:CHENNAMSETTY SUNEELMANOHARBABU; PATIL RAJENDRA; HAREL PRASHANT; HARIHARAN SIVARAMAKRISHNAN 权利人:PIRAMAL ENTPR LTD 摘要:The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R 1 has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.
专利号:WO-2014128523-A1 优先权日:2013-02-19 标 题 :A process for preparation of an intermediate of the pyrrolidine substituted flavones 发明人:CHENNAMSETTY SUNEELMANOHARBABU; BOKKA RAVISHANKAR; VEERAPPAN RATHINASAMI; SIVAKUMAR MEENAKSHI; HARIHARAN SIVARAMAKRISHNAN 权利人:PIRAMAL ENTPR LTD 摘要:The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.
专利号:US-2024262834-A1 优先权日:2021-05-28 标 题:Synthesis of btk inhibitor and intermediates thereof 发明人:CHEN YONGGANG; CORRY JAMES; DESMOND RICHARD; DI MASO MICHAEL J; FORSTATER JACOB H; KUETHE JEFFREY T; KUHL NADINE; LARSON REED; LEVESQUE FRANCOIS; NARSIMHAN KARTHIK; OTTE DOUGLAS; PRIER CHRISTOPHER K; SHEVLIN MICHAEL; SIROTA ERIC; TAN LUSHI; THAISRIVONGS DAVID A; TURNBULL BEN W H; WANG ZHIXUN; XIAO KAIJIONG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient synthetic processes useful in the preparation of Compound A, a BTK inhibitor of Formula (I): or a pharmaceutically acceptable salt thereof, including the preparation of intermediates used to make Compound A or a pharmaceutically acceptable salt thereof.
专利号:US-9487537-B2 优先权日:2013-06-12 标 题:Synthesis of isohexide dicarbamates and derivatives thereof 发明人:STENSRUD KENNETH 权利人:ARCHER DANIELS MIDLAND CO; ARCHER DANIELS MIDLAND CO 摘要:Dicarbamates of the reduction products of 2-hydroxymethyl-5-furfural (HMF) and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The dicarbamates of HMF-reduction products can serve as precursor materials from which various derivative compounds can be synthesized.
专利号:US-4301129-A 优先权日:1978-09-18 标题 :Synthesis of NaBH3 CN and related compounds 发明人:WADE ROBERT C; HUI BENJAMIN C 权利人:THIOKOL CORP 摘要:A process for the preparation of compounds of the formula RBH 3 CN wherein R is an alkali metal, a quaternary ammonium radical or a phosphonium radical wherein a compound of the formula RCN is treated with a stoichiometric amount or slightly less than a stoichiometric amount of a BH 3 donor is described. The final products are useful as hydrolysis stable reductants and as synthetic intermediates.
参考标题:An Original Catalytic Synthesis Of Boriran-1-Ols 作者:Leila O. Khafizova,Liliya I. Khusainova,Tat'Yana V. Tyumkina,Kirill S. Ryazanov,Natal'Ya R. Popod'Ko,Usein M. Dzhemilev |发布日期:2018.11 摘要:2-Alkylboriran-1-Ols Were Obtained In A One-Pot Process By Hydrolysis Of 1-Fluoro- And 1-Chloroboriranes In 90-92% Yield. The Starting 1-Haloboriranes Were Generated By Cycloboration Of α-Olefins With Bcl3.Sme2 Or Bf3.Thf In The Presence Of Mg Metal (Acceptor Of Halogen Ions) And Cp2Ticl2 Catalyst.
合成参考文献
摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 338.