Process for the preparation of oxazaphosphorine-2-amines
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United States of America Patent
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app pub date -
Dec 7, 2000
filing date -
Sep 6, 1997
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Abandoned
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Abstract
A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme 1 in which R.sub.1 is H, 2-bromoethyl, 2-chloroethyl, 2-hydroxyethyl, 2-mesyloxyethyl or 1-phenylethyl; R.sub.2 is H or 2-chloroethyl; R.sub.3 is H, 2-bromoethyl, 2-chloroethyl or 1-phenylethyl; and R.sub.4 is H; or R.sub.1 and R.sub.2, and also R.sub.3 and R.sub.4, together with the linked N atom, form an aziridide ring, where R.sub.1, R.sub.2 and R.sub.3 are not simultaneously H, and R.sub.1 and R.sub.3 are not simultaneously 1-phenylethyl; and Y, which is optionally present, is hydrogen chloride or hydrogen bromide. The reaction is carried out in a single vessel with phosphoryl chloride and an auxiliary base as an acid-binding agent with minimization of the effect of water and without isolation of an intermediate compound.
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