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:US-3558614-A 优先权日:1967-09-05 标题:Synthesis of tetranuclear dyes 发明人:JENKINS PHILIP W 权利人:EASTMAN KODAK CO 摘要:TETRANUCLEAR DYES DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4-THIONE AND A 2-IMIDAZOLIN-4-SELENONE ARE PREPARED IN GOOD YIELDS BY CONDENSING A QUATERNIZED MEROCYANINE DYE DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4-THIONE OR A 2-IMIDAZOLIN4-SELENONE WITH (1) A DIALKOXYALKYL ESTER OF AN ORGANIC ACID, (2) A TRIALKOXY ALKANE OR ARYL COMPOUND, (3) A 3,3-DIALKOZY-1ALKOXYPROPENE, (4) A 1-ANILINO-5-PHENYLIMINO-1,3-PENTADIENE OR (5) A SECOND QUATERNIZED MROCYANINE DYE DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4THIONE OR A 2-IMIDAZOLIN-4-SELENONE, EACH HAVING SUBSTITUTED ON THE CARBON IN THE 2-POSITION A GROUP SUCH AS A B-ACETANILIDOVINYL GROUP, A 4-ACETANILIDO-1,3-BUTADIENYL GROUP, AND A 6-ACETANILIDO-1,3,5-HEXADIENYL GROUP.
专利号:US-11261158-B2 优先权日:2017-11-17 标 题:Synthesis of 2-indolinone derivatives 发明人:PIISOLA ANTTI; TOIS JAN 权利人:FERMION OY 摘要:The present disclosure relates to a preparation method of methyl (E)-1-acetyl-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate from methyl 2-oxoindoline-6-carboxylate using high reaction temperatures and a reaction solvent enabling azeotropic removal of acetic acid during the reaction.
专利号:CN-111465594-A 优先权日:2017-11-17 标 题 :Synthesis of 2-indolinones known as intermediates for the preparation of nintedanib
专利号:US-11767302-B2 优先权日:2020-10-01 标题 :Reagents and methods for tetrazine synthesis 发明人:FOX JOSEPH M; LAMBERT WILLIAM; FANG YINZHI; AM ENDE CHRISTOPHER WILLIAM; MAHAPATRA SUBHAM; XIE YIXIN; WANG CHUANQI 权利人:UNIV DELAWARE 摘要:Disclosed herein are mono- and di-substituted tetrazines and methods of their preparation and converting an oxetanyl ester to a thio-substituted tetrazine, which is then converted to a mono-substituted tetrazine, a di-substituted tetrazine, or a vinylether disubstituted tetrazine.
专利号:US-2005215801-A1 优先权日:2002-06-28 标 题 :Process for preparation of optically active 1-substituted amino-2,3-epoxypropanes, intermediates for synthesis thereof and process for preparation of the intermediates 发明人:KITAJIMA KUMI; NAGASHIMA NOBUO 权利人:KITAJIMA KUMI; NAGASHIMA NOBUO 摘要:The present invention provides an industrial process for effectively and advantageously preparing optically active 1-substituted amino-2,3-epoxypropanes useful as intermediates for preparing agricultural chemicals and medical products from optically active 1-substituted amino-2,3-propanediols used as raw materials. The present invention also provides useful intermediates. Specifically, an optically active 1-substituted amino-2,3-propanediol (1) is reacted with an orthoacid ester (2) or thionyl chloride (3) to produce a cyclic optically active compound (4), and then a compound (5) containing a halogen atom is prepared by reaction with a ring-opening reaction agent having an ability to introduce a halogen atom X. Finally, an optical active 1-substituted amino-2,3-epoxypropane is prepared by ring-closure reaction in the presence of a base.