专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-9695169-B2 优先权日:2012-05-31 标 题:Synthesis of heterocyclic compounds 发明人:IBRAHIM PRABHA N 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.
专利号:US-2025034146-A1 优先权日:2023-07-13 标题:Electro-photochemical synthesis of 1,2,4-triazolo-[4,3-a]pyrazine 发明人:PIERCEY DAVIN GLENN; YOUNT JOSEPH ROBERT 权利人:PURDUE RESEARCH FOUNDATION 摘要:A method of preparing a 1,2,4-triazolo-[4,3-a]pyrazine backbone using an electro-photochemical process comprising coupling a compound comprising a 5-substituted tetrazole moiety to a compound comprising an optionally substituted pyrazine moiety electrochemically and subjecting the resulting compound to photochemical excitation with ultraviolet light.
专利号:US-4264527-A 优先权日:1979-08-01 标 题:Process for the preparation of cyclopropylmethyl-n-propylamine 发明人:CURTIS EDWYN A 权利人:CIBA GEIGY CORP 摘要:A process for preparing cyclopropylmethyl-n-propylamine from the reaction of cyclopropylmethylamine with propionitrile is described. The reaction takes place in the presence of a hydrogenation catalyst, preferably a mixture of rhodium on carbon and platinum on carbon. The process is particularly useful as it consumes the cyclopropylmethylamine by-product from another scheme for the synthesis of cyclopropylmethyl-n-propylamine.
专利号:US-5124460-A 优先权日:1991-05-06 标 题 :Enantioselective synthesis of 3-substituted 1-azabicyclo (2.2.1)heptanes 发明人:HUMPHREY GUY R 权利人:MERCK SHARP & DOHME 摘要:A process for preparing a substantially pure enantiomer of a compound formula (I) ##STR1## wherein X is O or S; and n R 2 represents hydrogen, --CF 3 , --OR 7 , --SR 7 , --NR 7 R 8 , --CN, --COOR 7 , --CONR 7 R 8 , or a saturated or unsaturated, substituted or unsubstituted hydrocarbon group, wherein R 7 and R 8 are independently selected from hydrogen and C 1-2 alkyl provided that --NR 7 R 8 is other than NH 2 ; n which process comprises cyclization of a compound of formula (10) or salt thereof: ##STR2## wherein X and R 2 are as defined in formula (I); and R 4 is a labile leaving group and optionally epimerizing the endo-diastereomer so prepared to produce the corresponding exo-diastereomer.
专利号:US-2018179191-A1 优先权日:2016-11-22 标题 :Synthesis of a compound that modulates the activity of bromodomain-containing proteins 发明人:SHEN JINYU; ST JULES MUSTAPHA; SPERANDIO DAVID; MOHAN SANKAR 权利人:GILEAD SCIENCES INC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n n n n n n n n n n or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.