乳酸甲酯置于四氯化碳,N-溴代丁二酰亚胺(Nbs)体系中,化学反应生成 3-溴丙酮酸乙酯 参考文献:Studies With N-Halo Reagents. Ii. New Syntheses Of β-Bromo-α-Keto Esters,Ethyl Phenylglyoxylate And Phenacyl Bromide Using N-Bromosuccinimide1 标题:Studies With N-Halo Reagents. Ii. New Syntheses Of β-Bromo-α-Keto Esters,Ethyl Phenylglyoxylate And Phenacyl Bromide Using N-Bromosuccinimide1 摘要: DOI:10.1021/ja01651A061
专利号:US-2025197904-A1 优先权日:2022-03-14 标 题 :A process for the synthesis of ( r)-2-(( tert-butoxycarbonyl)amino)-3-(diethoxyphosphoryl)propanoic acid or of phosphonate derivatives thereof 发明人:ABELE STEFAN; BROWN GARETH; MCINTYRE PETER; MIX Stefan 权利人:VIATRIS ASIA PACIFIC PTE LTD 摘要:The present invention relates to a process for the synthesis of (R)-2-((tert-butoxycarbonyl)amino)-3-(diethoxyphosphoryl)propanoic acid (“COMPOUNDâ€?), of phosphonate derivatives thereof, or of salts of any of the aforementioned; to a crystalline form of COMPOUND, and to the use of COMPOUND (especially of COMPOUND in crystalline form) or phosphonate derivatives or salts thereof for the preparation of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester (also known as selatogrel), or of a pharmaceutically acceptable salt thereof.
专利号:US-9475814-B2 优先权日:2011-10-03 标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof 发明人:HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC 权利人:EUROSCREEN SA 摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
专利号:US-6262272-B1 优先权日:1997-11-13 标题 :Method of synthesis of pyrrole amides 发明人:RAGAN JOHN ANTHONY; MAKOWSKI TERESA WOODALL; AM ENDE DAVID JON; CLIFFORD PAMELA JANE; YOUNG GREGORY RANDALL; CONRAD ALYSON KAY; EISENBEIS SHANE ALLEN; QUALLICH GEORGE JOSEPH; ALLEN DOUGLAS JOHN MELDRUM 权利人:PFIZER 摘要:A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakane-diones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.
专利号:US-5684185-A 优先权日:1992-10-01 标题 :Process for the stereoselective synthesis of 3-substituted 2-sulfonylmethylpropionic acids, and intermediate products 发明人:BECK GERHARD; JENDRALLA JOACHIM-HEINER; KAMMERMEIER BERNHARD 权利人:HOECHST AG 摘要:Compounds of the formula I ##STR1## can be prepared in a multi-day process starting from the compounds of the formulae II and III n n R.sup.1 --SH, II n n ##STR2## where the substituents R 1 , R 2 and R 3 have the meanings given.
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:US-4316029-A 优先权日:1979-06-22 标 题:Synthesis of vincaminic acid derivatives 发明人:ROSSEY GUY 权利人:SYNTHELABO 摘要:Vincaminic acid derivatives of formula (A) ##STR1## useful in treating cerebral insufficiency, are prepared by reacting 1-ethyl-2,3,4,6,7,12-hexahydroindolo[2,3-a]quinolizine with the 2,4-DNP hydrazone of ethyl or methyl bromopyruvate followed by (i) reduction of the Câ•?N bond and (ii) simultaneous cyclization with removal of the ketone-protecting group in either order.
参考文献:10.1107/s1600536811017077 摘要:Dahmani S, Kandri Rodi Y, Luis SV, Essassi el M, El Ammari L. Ethyl 8-amino-6-bromoimidazo[1,2-a]pyridine-2-carb-oxy-late. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1390.