Process for preparation of aryl phosphorous compounds

摘要

The present invention relates to cost effective, transition-metal-free one pot process for the preparation of aryl phosphorous compounds of formula (I). Particularly, the present invention provides a process for C—P bond formation. In particular, the invention relates to mild fluoride induced generation of aryne species in situ which allows P—C bond formation to obtain aryl phosphorous compounds of formula (I) under mild condition.

主权项

1. A one pot process for the preparation of aryl phosphorous compound of formula (I) comprising reacting o-(trimethylsilyl) aryl triflates (formula II) with phosphorous compound of formula (III) in presence of CsF in polar solvent under stirring for a period ranging between 4-35 h, concentrating and purifying to obtain aryl phosphorous compound of formula (I); wherein, R represents hydrogen, alkyl, alkenyl, alkynyl, halo, hydroxy, alkoxy, (un)substituted or substituted aryl, benzyl, (un)substituted or substituted heteroaryl, oxalane group, —O—CH2—CH2—O—; N—R R′ and R″ represent alkyl, benzyl, alkenyl, alkynyl, (un)substituted or substituted aryl, (un)substituted or substituted heteroaryl; ‘n’ is 0-2; ‘m’ is 0-2; with the proviso, when ‘m’ is 0, ‘n’ is 2; R represents hydrogen, alkyl, alkenyl, alkynyl, halo, hydroxy, alkoxy, (un)substituted or substituted aryl, benzyl, (un)substituted or substituted heteroaryl, oxalane group, —O—CH2—CH2—O, N—R and R′ represent alkyl, benzyl, alkenyl, alkynyl, (un)substituted or substituted aryl, (un)substituted or substituted heteroaryl; with the proviso, when ‘n’ is 1, ‘m’ is 1; R represents hydrogen, alkyl, alkenyl, alkynyl, halo, hydroxy, alkoxy, (un)substituted or substituted aryl, benzyl, (un)substituted or substituted heteroaryl, oxalane group, —O—CH2—CH2—O, N—R and R″ represent alkyl, benzyl, alkenyl, alkynyl, (un)substituted or substituted aryl, (un)substituted or substituted heteroaryl; with the proviso, when ‘n’ is 0, ‘m’ is 2; R represents hydrogen, alkyl, alkenyl, alkynyl, halo, hydroxy, alkoxy, (un)substituted or substituted aryl, benzyl, (un)substituted or substituted heteroaryl, oxalane group, —O—CH2—CH2—O, N—R and R″ represent alkyl, benzyl, alkenyl, alkynyl, (un)substituted or substituted aryl, (un)substituted or substituted heteroaryl.