Process for the preparation of phosphitylation agents

Details Process for the preparation of phosphitylation agents Process for the preparation of phosphitylation agents

C - Chemistry, Metallurgy

07

F

C07F 9/26 (2006.01) C07F 9/24 (2006.01)

Patent

CA 2510473

A process for the preparation of a compound of formula R1-Y1-P(NR2R3 )2 is provided. The process comprises reacting a compound of formula PX3 with a compound of formula HNR2R3 to form a compound of formula X-P(NR2R3)2; and reacting the compound of formula X-P(NR2R3)2 with a compound of formula R1-Y1- H in the presence of a hydrocarbon solvent to form the compound of formula R1- Y1-P(NR2R3 )2. R1 represents a phosphorus protecting group; R2 and R3 each independently represent an alkyl, preferably a C1-6alkyl, group, or R2 and R3 are joined, together with the N to which they are attached, to form a 5-7 membered ring; Y1 represents O or S, preferably O; and X represents a halogen, preferably Cl. The preferred solvent is toluene.

L'invention concerne un procédé de préparation d'un composé de formule R?1¿-Y?1¿-P(NR?2¿R?3¿ )¿2?. Ce procédé consiste à faire réagir un composé de formule PX¿3? avec un composé de formule HNR?2¿R?3¿ pour former un composé de formule X-P(NR?2¿R?3¿)¿2? et à faire réagir le composé de formule X-P(NR?2¿R?3¿)¿2? avec un composé de formule R?1¿-Y?1¿-H en présence d'un solvant hydrocarburé pour former le composé de formule R?1¿-Y?1¿-P(NR?2¿R?3¿ )¿2?. R?1¿ représente un groupe protecteur phosphoré ; R?2¿ et R?3¿ représentent chacun indépendamment un alkyle, de préférence un groupe alkyle en C¿1-6?, ou R?2¿ et R?3¿ sont assemblés, avec le N auquel ces derniers sont attachés, pour former un cycle à 5-7 chaînons ; Y?1¿ représente O ou S, de préférence O, et X représente un halogène, de préférence Cl. Le solvant préféré est le toluène.

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