专利号:US-11649213-B2 优先权日:2018-09-26 标题 :Synthetic method for the preparation of a 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol compound 发明人:MEISENBACH MARK; MARTIN BENJAMIN; RONDE NIEK JOHANNES; RUIZ CARMEN 权利人:MEREO BIOPHARMA 1 LTD 摘要:Provided is a process for preparing a compound, comprising the steps of a) Reacting a compound of Formula A (Formula A) with the compound 3 (3) to provide the compound 5 (5) or a salt or solvate thereof, wherein R is a linear or branched C1-C5 alkyl. Further provided is the compound 5 or a salt or solvate thereof. (5) The use of these compounds in the synthesis of 3-[5-Amino-4-(3-Cyanobenzoyl)-Pyrazol-1-yl]-N-Cyclopropyl-4-Methylbenzamide is also provided.
专利号:US-5541322-A 优先权日:1994-10-14 标题:Synthesis of 6-azaandrostenones 发明人:FANG FRANCIS G; SHARP MATTHEW J 权利人:GLAXO WELLCOME INC 摘要:A process of providing novel compounds of Formula (I), that are useful as 6-azaandrostenone testosterone 5-alpha-reductase inhibitors, from commercially available compounds of Formula (II) ##STR1## wherein the substituents are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof.
专利号:US-3992436-A 优先权日:1976-01-02 标题:Synthesis of oxalate esters from carbon monoxide and carboxylic ortho esters 发明人:ZEHNER LEE R 权利人:ATLANTIC RICHFIELD CO 摘要:A process for the preparation of oxalate esters by the catalytic oxidative carbonylation of carboxylic ortho esters with carbon monoxide and oxygen-containing gas in the presence of a metal salt catalyst, an amine base and a catalytic amount of an alcohol. Preferably a catalytic amount of particular metal oxidizing salts is employed along with a catalytic amount of an acid or an amine salt compound. Alternatively various counterions and ligands of the metal salt catalysts may be employed.
专利号:US-6953678-B1 优先权日:1999-07-26 标题 :Use of orthoesters for the synthesis of chiral acids in biocatalyzed irreversible esterification processes 发明人:MORRONE RAFFAELE; NICOLOSI GIOVANNI; PIATTELLI MARIO 权利人:CONSIGLIO NAZIONALE RICERCHE 摘要:A process for the resolution of enantiomeric mixtures of a chiral carboxylic acid, including an esterification reaction of the carboxylic acid in an organic solvent, in the presence of a stereoselective hydrolase, characterized in that an orthoester of the formula R 1 —C(OR 2 ) 3 , in which R 1 is selected from H and C 1 –C 4 alkyl and R 2 is C 1 –C 8 alkyl or —CH 2 —C 6-10 aryl, is used as the esterification reactive.
专利号:US-4237055-A 优先权日:1979-06-18 标 题 :Synthesis of 1RS,4SR,5RS-4-(4,8-dimethyl-5-hydroxy-7-nonen-1-yl)-4-methyl-3,8-dioxabicyclo[3.2.1]octane-1-acetic acid 发明人:HAJOS ZOLTAN G; WACHTER MICHAEL P 权利人:ORTHO PHARMA CORP 摘要:A method of synthesizing 1RS,4SR,5RS-4-(4,8-dimethyl-5-hydroxy-7-nonen-1-yl)-4-methyl-3,8-dioxabicyclo [3.2.1]octane-1-acetic acid. The acid is a derivative of the natural product zoapatanol, one of the active ingredients in the zoapatle plant, and is active as a utero-evacuant agent.
专利号:US-4990631-A 优先权日:1990-05-30 标 题:Process for the preparation of 2,2-dialkoxy cyclic ortho esters derived from lactones 发明人:ALSTER KAROL 权利人:ALZA CORP 摘要:This invention is directed to a process for the synthesis of 2,2-dialkoxy cyclic ortho esters derived from lactones which comprises reacting trialkyl orthoformate with boron trifluoride to give dialkoxymethylium tetrafluoroborate; reacting dialkoxymethylium tetrafluoroborate with a lactone to give the corresponding O-alkyllactonium tetrafluoroborate; and reacting the O-alkyllactonium tetrafluoroborate with an alkoxide, or alternatively with an alkanol in the presence of a base; wherein the first two steps of the process of the invention are conducted in the absence of solvents, other than the reactants themselves. The third step may also optionally be run without solvents. n The invention is also directed to the preparation of the O-alkyllactonium tetrafluoroborate in one reaction vessel; that is, the boron trifluoride is added to the trialkyl orthoformate and the lactone in a single reaction vessel. As the intermediate dialkoxymethylium tetrafluoroborate is formed, it reacts in situ with the lactone in the reaction mixture, thus avoiding the additional steps of separating the dialkoxymethylium tetrafluoroborate and then reacting it with the lactone in a separate step and vessel.
摘要:Nógrádi, M., Science of Synthesis, (2003) 14, 218. 摘要:Zhang, M.; Hanson, P. R., Science of Synthesis, (2007) 20, 912. 摘要:von Angerer, S.; Warriner, S. L., Science of Synthesis, (2007) 29, 304.