专利号:US-3872168-A 优先权日:1972-10-02 标题:Synthesis of acids and amides 发明人:COLLMAN JAMES P; WINTER STANLEY R; KOMOTO ROBERT G 权利人:TRUSTEES OF THE LELAND STAMFOR 摘要:Synthesis of acids R1COOH and amides R1CONR2R3 wherein R1 is attached to the carbonyl group by an aliphatic carbon atom and R2 and R3 are hydrogen or organic groups of a primary or secondary amine, by forming an alkyl or acyl intermediate (R1Fe(CO) 4 or R1COFe(CO) 4) and treating the intermediate with a suitable cleaving agent and, in the case of amides, also with ammonia or an amine.
专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-5118853-A 优先权日:1988-10-13 标题:Processes for the synthesis of 3-disubstituted aminoacroleins 发明人:LEE GEORGE T; REPIC OLJAN 权利人:SANDOZ LTD 摘要:Process for the synthesis of compounds of the formula ##STR1## comprising the steps of (i) reacting a compound of the formula ##STR2## with oxalyl chloride or oxalyl bromide to form the corresponding compound of the formula ##STR3## (ii) reacting said compound of the formula ##STR4## with a compound of the formula ##STR5## to form the corresponding compound of the formula ##STR6## (iii) hydrolyzing said compound of the formula ##STR7## to obtain the corresponding compound of the formula ##STR8## the use of the compounds of the formula ##STR9## for the synthesis of the compounds of the formula ##STR10## and the use of the intermediates of Formula VII for the direct synthesis of the compounds of Formula II, n wherein n R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 1b is phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n one of R 3 and R 4 is ##STR11## and the other is primary or secondary C 1-6 alkyl not containing an asymmetric carbon atom, C 3-6 cycloalkyl or phenyl-(CH 2 ) m -, n wherein n R 7 is hydrogen, C 1-3 alkyl, n-butyl, i-butyl, t-butyl, C 1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 8 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 9 is hydrogen, C 1-2 alkyl, C 1-2 alkoxy, fluoro or chloro, and n m is 1, 2 or 3, with the provisos that not more than one of R 7 and R 8 is trifluoromethyl, not more than one of R 7 and R 8 is phenoxy, and not more than one of R 7 and R 8 is benzyloxy, n R 5 is hydrogen, C 1-3 alkyl, n-butyl, i-butyl, t-butyl, C 3-6 cycloalkyl, C 1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, and n R 6 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, or benzyloxy, with the provisos that not more than one of R 5 and R 6 is trifluoromethyl, not more than one of R 5 and R 6 is phenoxy, and not more than one of R 5 and R 6 is benzyloxy, n R 10 is C 1-6 alkyl, each X is chloro or bromo, and each X.sup.⊖ is chloride or bromide.
专利号:US-11891351-B2 优先权日:2020-03-20 标 题 :Synthesis of capsaicin derivatives 发明人:LAGER ERIK 权利人:AXICHEM AS 摘要:The present invention relates to the synthesis of capsaicin derivatives, specifically to the synthesis of 6-heptyne derivatives of capsaicin.
专利号:US-2021107859-A1 优先权日:2018-04-06 标题 :A process for the synthesis of carbon labeled organic compounds 发明人:AUDISIO DAVIDE; CANTAT THIBAULT; DESTRO GIANLUCA 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A process for the synthesis of a carbon labeled organic compound containing a carbon labeled carboxyl group is described. A method of using carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; a process for manufacturing labeled pharmaceuticals and agrochemicals comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; and a process for producing tracers comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure are also described.
参考文献:10.1186/1556-276x-6-449 摘要:Choi B, Pak Y, Kim KS, Lee K, Jung G. Simultaneous fabrication of line defects-embedded periodic lattice by topographically assisted holographic lithography. Nanoscale Research Letters. 2011 Jul 12;6(1):449. doi: 10.1186/1556-276x-6-449. 参考文献:10.1107/s1600536811005022 摘要:Liu F, Zhang F, Chen Q, Dong M. (Z)-N′-Hydroxy-4-(trifluoromethyl)benzimidamide. Acta Crystallogr E Struct Rep Online. 2011 Mar 12;67(4):o859. doi: 10.1107/s1600536811005022. 参考文献:10.1107/s1600536811009597 摘要:Betz R, Gerber T. 2-(Trifluoro-meth-yl)benzoic acid. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o907. 参考文献:10.1107/s1600536811011731 摘要:Giffin NA, Hendsbee AD, Masuda JD. A new polymorph of 2,6-bis-(trifluoro-meth-yl)benzoic acid. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1054.