📜1-甲基-4-哌啶酮-3-羧酸甲酯置于盐酸,异戊醇,水,Sodium体系中,化学反应生成 4-氨基-1-甲基哌啶 参考文献:Tomita,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1951,Vol. 71,P. 1053,1057 标题:Tomita,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1951,Vol. 71,P. 1053,1057
专利号:US-5516891-A 优先权日:1992-06-16 标题:Liquid phase synthesis of peptides and peptide derivatives 发明人:SIWRUK GARY A; EYNON JOHN S 权利人:KINERTON LTD 摘要:PCT No. PCT/US93/05783 Sec. 371 Date May 25, 1994 Sec. 102(e) Date May 25, 1994 PCT Filed Jun. 16, 1993 PCT Pub. No. WO93/25571 PCT Pub. Date Dec. 23, 1993.A liquid phase peptide synthetic method which uses (1) Fmoc as the protecting group for the non-side chain amino functionality, (2) ammonia, a primary or secondary amine to remove the Fmoc protecting group, and (3) substituted carbodiimide as the coupling agent for the C to N synthesis of peptides or peptide derivatives in a proper organic solvent.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:WO-2023213264-A1 优先权日:2022-05-05 标 题 :Synthesis of amide compound and use thereof 发明人:WANG ZHAOYIN; ZHANG JIAN; CAO JINRUI 权利人:SHANGHAI INST ORGANIC CHEMISTRY CAS 摘要:The present invention relates to a novel oleanamide derivative for activating a KEAP/NRF2/ARE signaling pathway. The compound of the present invention is represented by general formula (I), wherein L, R 3 , R 4 , Z, and n are set forth in the description specification and the claims. Also disclosed are a method for preparing the compound represented by general formula I and an activity test result thereof for activating the KEAP/NRF2/ARE signaling pathway. The compound represented by general formula (I) of the present invention can be used for treating and preventing multiple sclerosis (MS), Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), Friedreich's ataxia (FRDA), spinal muscular atrophy (SMA), neuromyelitis optica (NMO), spinocerebellar ataxia (SCA), and other neurodegenerative diseases, and can also be used for treating cerebral apoplexy, autoimmune diseases, diabetes, kidney diseases, and other chronic diseases.
专利号:US-11319288-B2 优先权日:2018-04-26 标 题:Method for the preparation of pimavanserin base 发明人:NOVO BARBARA; BONANOMI JACOPO; BERTOLOTTI MATTIA 权利人:OLON SPA 摘要:Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).
专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-10807953-B2 优先权日:2015-03-02 标题:Processes and intermediates for the preparation of Pimavanserin 发明人:BILJAN TOMISLAV; DOGAN JASNA; METSGER LEONID; PIPERCIC SARA MORASI; RATKAJ MARINA; SKUGOR MAJA MATANOVIC; WANG YI 权利人:PLIVA HRVATSKA D O O 摘要:The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
参考文献:10.1055/s-0036-1588303 摘要:Rossi R, Bellina F, Lessi M, Manzini C, Marianetti G. Direct (Hetero)arylation Reactions of (Hetero)arenes as Tools for the Step- and Atom-Economical Synthesis of Biologically Active Unnatural Compounds Including Pharmaceutical Targets. Synthesis. 2016 Oct 11;48(22):3821–62. doi: 10.1055/s-0036-1588303.