| 摘要 |
A process for the preparation of a compound of formula R<SUP>1</SUP>-Y<SUP>1</SUP>-P(NR<SUP>2</SUP>R<SUP>3</SUP>)<SUB>2 </SUB>is provided. The process comprises reacting a compound of formula PX<SUB>3 </SUB>with a compound of formula HNR<SUP>2</SUP>R<SUP>3 </SUP>to form a compound of formula X-P(NR<SUP>2</SUP>R<SUP>3</SUP>)<SUB>2</SUB>; and reacting the compound of formula X-P(NR<SUP>2</SUP>R<SUP>3</SUP>)<SUB>2 </SUB>with a compound of formula R<SUP>1</SUP>-Y<SUP>1</SUP>-H in the presence of a hydrocarbon solvent to form the compound of formula R<SUP>1</SUP>-Y<SUP>1</SUP>-P(NR<SUP>2</SUP>R<SUP>3</SUP>)<SUB>2</SUB>. R<SUP>1 </SUP>represents a phosphorus protecting group; R<SUP>2 </SUP>and R<SUP>3 </SUP>each independently represent an alkyl, prefer-ably a C<SUB>1-6</SUB>alkyl, group, or R<SUP>2 </SUP>and R<SUP>3 </SUP>are joined, together with the N to which they are attached, to form a 5-7 membered ring; Y<SUP>1 </SUP>represents O or S, preferably O; and X represents a halogen, preferably Cl. The preferred solvent is toluene.
|
