专利号:US-9115128-B2 优先权日:2013-06-06 标 题 :Compounds of 3-(5-substituted Oxy-2, 4-dinitrophenyl)-2-oxo-propionic acid ester, synthesis and applications thereof 发明人:PUTHIAPARAMPIL TOM THOMAS; SAMBASIVAM GANESH; GOVINDA RAJULU GAVARA; KORAMANGALA RAVINDRA CHANDRAPPA 权利人:ANTHEM BIOSCIENCES PVT LTD; ANTHEM BIOSCIENCES PVT LTD 摘要:Synthesis of the novel compound 3 (3-(5-substituted Oxy-2,4-dinitro-phenyl)-2-oxo-propionic acid ester) to make Pyrroloquinoline quinone (PQQ) and using it for pharmaceutical purposes is described. More specifically, this disclosure relates to synthesizing the PQQ in an efficient method by using a novel intermediate Formula 1 resulting in a shorter process and higher yield of PQQ. A unique process to make sodium compound of PQQ using either sodium hydroxide and/or sodium carbonate is also shown.
专利号:US-2025115551-A1 优先权日:2023-10-03 标 题:Synthesis of ras inhibitors 发明人:LI YI; MENDOZA BENJAMIN; NAGANATHAN SRIRAM; WANG ROSS; YI YI; BALLMER STEVEN G; DAVIDSON JAMES; HUANG XIAOJUN 权利人:REVOLUTION MEDICINES INC 摘要:The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.
专利号:US-10266467-B2 优先权日:2017-08-02 标 题:Synthesis of glycols via transfer hydrogenation of alpha-functional esters with alcohols 发明人:CHAKRABORTY SUMIT; HEMBRE ROBERT THOMAS 权利人:EASTMAN CHEM CO 摘要:A transfer hydrogenation process for forming vicinal diols by hydrogenating 1,2-dioxygenated organic compounds using alcohols as the reducing agent instead of the traditional H 2 gas. The transfer hydrogenation is carried out under milder conditions of temperature and pressure than is typical for ester hydrogenation with H 2 . The milder conditions of operation provide benefits, such as lower operating and capital costs for industrial scale production as well as savings in product purification due to the avoidance of by-products from exposure of reaction mixtures and products to high temperatures.
专利号:US-3708477-A 优先权日:1968-06-27 标 题:Process of total synthesis of cephalosporin derivatives and intermediates 发明人:MARTEL J; HEYMES R 权利人:ROUSSEL UCLAF 摘要:PROCESS FOR THE PREPARATION OF RACEMIC OR OPTICALLYACTIVE CEPHALOSPORINE DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-NH2-2-CEPHEM WHEREIN R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED AKYL, ARYL AND SUBSTITUTED ARYL, WHICH COMPRISES THE STEPS OF REACTING AN AMINO ACID OF THE FORMULA R1-NH-CH2-CH2-COOH WITH BENZYL ALCOHOL, CONDENSING THE BENZYL ESTER THUS OBTAINED WITH AN OXALATE, CONVERTING THE BENZYL ESTER OF 2,3DIOXI-4-CARBOXY-PYRROLIDINE INTO THE CORRESPONDING ACID, SUBJECTING SAID ACID TO AMINOMETHYLATION, THUS YIELDING A COMPOUND OF THE FORMULA 1-R1,3-OH,4-(R'-N(-R'')-CH2-)PYRROL-3-IN-2-ONE CONVERTING SAID COMPOUND INTO THE CORRESPONDING 4-ACYLTHIOMETHYL DERIVATIVE, CONVERTING SAID DERIVATIVE INTO THE CORRESPONDING 4-THIOMETHYL DERIVATIVE, CONDENSING SAID DERIVATIVE WITH AN ENAMINE OF THE FORMULA R-OOC-C(-Y)=CH-NH2 TO OBTAIN A THIAZINE DERIVATIVE OF THE FORMULA 2-(Y-CH(-COO-R)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-D)-1,3-THIAZIN-4-ONE CONVERTING SAID THIAZINE DERIVATIVE INTO A COMPOUND OF THE FORMULA 2-(H2N-CH(-COOH)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-)-1,3-THIAZIN-4-ONE SUBJECTING SAID COMPOUND TO THE ACTION OF A TRITYLATION AGENT, RECOVERING THE THREO ISOMER OF THE TRITYLATED DERIVATIVE, LACTAMIZING SAID THREO ISOMER TO OBTAIN THE Y-LACTAM OF DL-6H,7H-CIS-7-TRITYLAMINO-3-AMINOALKYL-CEPH 3-EME-4-CARBOXYLIC ACID, DETRITYLATING SAID Y-LACTAM AND RECOVERING SAID RACEMIC OF OPTICALLY ACTIVE CEPHALOSPORIN DERIVATIVES. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF THE CORRESPONDING 7ACYLAMINO DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-(R2-NH-)-2-CEPHEM WHEREIN R1 HAS THE ABOVE DEFINITION AND R2 IS THE ACYL OF AN ORGANIC CARBOXYLIC ACID WHICH COMPOUNDS ARE ALSO PART OF THE INVENTION AND ARE USEFUL AS ANTIBIOTICS.
专利号:US-2019039978-A1 优先权日:2017-08-02 标 题:Synthesis of glycols via transfer hydrogenation of alpha-functional esters with alcohols
专利号:EP-3661901-B1 优先权日:2017-08-02 标 题:Synthesis of glycols via transfer hydrogenation of alpha-functional esters with alcohols
参考标题:A One-Step Synthesis Of Alkyl 2-Oxo-3-Alkenoates From Alkenyl Grignard Reagents And Dialkyl Oxalates 作者:M. Rambaud,M. Bakasse,G. Duguay,J. Villieras 摘要:The Reaction Of Alkenyl Grignard Reagents With Dialkyl Oxalates At 80°C In An Ether/tetrahydrofuran Mixture (1:1) Leads To The Formation Of The Corresponding Alkyl 2-Oxo-3-Alkenoates In High Yields. Thus A Mild And Convenient One-Step Synthesis Of 3-Isopropenyl-Substituted 2-Oxoesters Is Described.
合成参考文献
摘要:Masse, C. E., Science of Synthesis, (2007) 20, 988.