Preparation of diazapentalene derivatives via epoxydation of...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01)

Patent

CA 2616303

The present invention relates to a process for preparing a compound of formula (I), wherein R1 Is Pg1 Or P1~; P1' is CO-hydrocarbyl; P2 is CH2, O or N-Pg2; and Pg 1 and Pg 2 are each independently nitrogen protecting groups; (i) reacting a compound of formula (II) with a dioxirane to form an epoxide of formula (III); where X is selected from CN, CH2N3, CH2NH-Pg2, ONH-Pg2, NHNH- Pg2, N(Pg2)NH-Pg2; (ii) converting a compound of formula (III) to a compound of formula (I).

La présente invention concerne un procédé pour préparer un composé répondant à la formule (I), dans laquelle R1 représente Pg1 ou P1' ; P1' représente un groupe CO-hydrocarbyle ; P2 représente CH2, O ou N-Pg2 ; et Pg1 et Pg2 représentent chacun indépendamment des groupes protecteurs d'azote ; le procédé comprenant les étapes consistant à (i) mettre à réagir un composé répondant à la formule (II) avec un dioxiranne pour former un époxyde répondant à la formule (III) ; X étant choisi parmi CN, CH2N3, CH2NH-Pg2, ONH-Pg2, NHNH-Pg2, N(Pg2)NH-Pg2 ; (ii) convertir un composé répondant à la formule (III) en un composé répondant à la formule (I).

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