乙酸乙酯置于乙醚,氨,Sodium Amide体系中,化学反应生成丙二酸单乙酯 参考文献:Hauser; Levine; Kibler,Journal Of The American Chemical Society,1946,Vol. 68,P. 27 标题:Hauser; Levine; Kibler,Journal Of The American Chemical Society,1946,Vol. 68,P. 27
专利号:US-4870199-A 优先权日:1986-04-30 标题 :Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 发明人:CHEN KAU-MING; HARDTMANN GOETZ E; KAPA PRASAD K; LEE GEORGE T; LINDER JEROME; WATTANASIN SOMPONG 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Process for the synthesis of compounds of the formula in R[R*,S*] enantiomeric form, wherein each P1 is independently an hydroxy group-protecting group, and R2z is C1-4alkyl, benzyl or allyl, comprising, as a key step when R2z is R2x, the reaction of the compound of the formula in (S) enantiomeric form with a compound of the formula Mg &cir& +2 ((-)OOC-CH2-COOR2x)2 to obtain a compound of the formula in (S) enantiomeric form, and, as a key step when R2z is R2y, the reaction of a compound of the formula in (S) enantioimeric form with a compound of the formula Li(+)(-)CH2-COOR2y to obtain a compound of the formula in (S) enantiomeric form, wherein R2x is primary or secondary C1-4alkyl, benzyl or allyl, R2y is C1-4alkyl not containing an asymmetric carbon atom, and R3' is methyl or ethyl, processes for the synthesis of compounds of the formula comprising reacting a compound of the formula with the reaction product of a strong base and a compound of the formula optionally followed by, when R2z is allyl, cleavage of the allyl and P1 groups to obtain the corresponding compound of the formula wherein each R7 is methyl or ethyl, R is as defined in the specification, and each P1 independently and R2z are as defined above, and the compounds of the formula wherein R and each R7 are as defined above.
专利号:US-7368568-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:EP-4186890-A1 优先权日:2021-11-29 标题 :Preparation of n-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide for the synthesis of tirbanibulin 发明人:ARE CELESTE; BALLETTE ROBERTO; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:The present invention relates to a process for the preparation of N-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide, which is a suitable intermediate for the synthesis of tirbanibulin or a pharmaceutically acceptable salt thereof, as well as to a process for the preparation of tirbanibulin or a pharmaceutically acceptable salt thereof using said N-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide intermediate.
专利号:US-5124478-A 优先权日:1987-12-22 标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 发明人:BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER 权利人:HOECHST AG 摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.
专利号:US-6933385-B2 优先权日:2001-08-03 标题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:SCHERING AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:EP-2231627-B1 优先权日:2007-12-03 标题 :New process for the synthesis of moguisteine 发明人:VIGANO' ENRICO; ARRIGHI MASSIMILIANO; MOLTENI RENATO; LANFRANCONI SIMONA; LANDONIO ERNESTO 权利人:A M S A ANONIMA MATERIE SINT E AFFINI S P A 摘要:The invention relates to a process for the synthesis of moguisteine that is ethyl ester of (R,S)-3-[2-[(2-methoxyphenoxy)methyl]-1,3-thiazolidin-3-yl]-3-oxypropanoic acid which comprises the steps of forming a new cyclic intermediate of formula 2-[(2-methoxyphenoxy)methyl]-1,3-dioxolane (4), forming (R,S)-2-[(2-methoxyphenoxy)methyl]-1,3-thiazolidine (6) and reacting this latter with monoethylmalonic acid (7) or a salt thereof. The moguisteine of the invention is obtained in high yield and purity.
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 227. 摘要:M. Levy and P. J. Magoulas, J. Am. Chem. Soc. 84, 1345 (1962). 摘要:P. K. Glasoe and J. R. Hutchison, J. Phys. Chem. 68, 1562 (1964). 摘要:Yang, Z.; Dong, K., Science of Synthesis: Knowledge Updates, (2024) 2, 246. 摘要:Liao, L.; Zhang, Y.; Yu, J.-S., Science of Synthesis: Knowledge Updates, (2024) 1, 240.