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Merck Sharp and Dohme Corp
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Schering Corp
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Publication date
Application filed by Schering CorpfiledCriticalSchering Corp
Publication of ES544744A0publicationCriticalpatent/ES544744A0/es
Publication of ES8608525A1publicationCriticalpatent/ES8608525A1/es
Organic Low-Molecular-Weight Compounds And Preparation Thereof
(AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions
(AREA)
Abstract
METODO DE OBTENCION DEL ACIDO 5R,6S,8R-6-(1-HIDROXIETIL)-2-(2-CARBAMOILOXIETILTIO)-PENEM-3-CARBOXILICO. CONSISTENTE EN LA REACCION DE UN COMPUESTO DE FORMULA (I) DONDE CUALQUIER GRUPO FUNCIONAL PUEDE SER OPCIONALMENTE PROTEGIDO; CON UN COMPUESTO DE ORGANOFOSFORO TRIVALENTE(TRIETILFOSFITO); UTILIZANDO COMO MEDIO DE REACCION UN DISOLVENTE INERTE (TOLUENO, BENCENO, ETERES, ETC...) Y BAJO UNA TEMPERATURA COMPRENDIDA ENTRE 20J Y 80JC, DURANTE UN PERIODO DE TIEMPO DE 6-24 H. POSTERIORMENTE Y DE FORMA ALTERNATIVA, SOMETER EL COMPUESTO OBTENIDO A UNO DE LOS PROCESOS SIGUIENTES: DESPROTECCION DE GRUPOS PROTEGIDOS; SEPARACION DEL ESTEREOISOMERO (5R,6S,8R); CONVERSION DE UN ACIDO LIBRE EN UNA SAL O UN ESTER METABOLIZABLE; CONVERSION DE UNA SAL O ESTER EN UN ACIDO LIBRE; TRANSESTERIFICACION DE UN ESTER O CONVERSION DE UN ESTER EN UNA SAL; CONVERSION DE UNA SAL A OTRA O EN UN ESTER.
Analogifremgangsmaate for fremst av terapeutisk aktiv (4r,5s,6s,8r,2's,-4's)-3- 4-(dimethylamino-carbonyl)-pyrrolidinhylthio -4-methyl-6-(1-hydroxyethyl)-1-azabicyclo- 3,2,0 hept-2-en-7-on-2-carboxylsyre i krystallinsk form.