📜苯基亚甲基双(三环己基磷)二氯化钌,1,3-Bis(2,4,6-Trimethylphenyl)-4,5-Dihydroimidazolium Chloride 在 Potassium 2-Methylbutan-2-Olate体系中,用 正己烷,甲苯作为反应溶剂,反应 18.17H,以50%的收率获得[1,3-Bis(2,4,6-Trimethylphenyl)Imidazolidin-2-Ylidene]-Dichloro-(3-Phenylinden-1-Ylidene)Ruthenium,Tricyclohexylphosphane 参考文献:Preparation Of Epothilone Derivatives 标题:Preparation Of Epothilone Derivatives 摘要:该发明涉及一种新型工艺,用于制备式i的环丙沙星衍生物,其中r1和r2各自独立地表示氢或保护基,R3为甲基或三氟甲基,这些衍生物在合成式iv的去氧环丙沙星衍生物的前体中有用,其中r3为甲基或三氟甲基.式iv的去氧环丙沙星具有抑制肿瘤细胞生长的作用,因此是新型抗癌药物的有前途的候选药物.
专利信息
专利号:US-9328108-B2 优先权日:2011-10-28 标 题 :Process for preparing an intermediate of the macrocyclic protease inhibitor TMC 435 发明人:HORVATH ANDRAS; WUYTS STIJN; DEPRÉ DOMINIQUE PAUL MICHEL; COUCK WOUTER LOUIS J; CUYPERS JOZEF LUDO JAN; HARUTYUNYAN SYUZANNA; BINOT GREGORY FABIEN SEBASTIAN 权利人:JANSSEN PHARMACEUTICALS INC 摘要:The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,12aR,14aR)-cyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxy-8-methyl-2-[4-(1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
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