Benzyl cyanoacetals
AssigneeBurroughs Wellcome Co.
InventorsDavid A. Yeowell, Roy A. Swaringen, Jr.
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Abstract
Benzyl cyanoacetals of formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is a halogen or a hydrogen atom, an alkoxy group, an alkyl group, or a dialkylamino group; R.sup.4 is an alkoxycarbonyl group, or an aldehyde group; And R.sup.5 is an alkyl group; the alkyl or alkoxy groups each having from 1 to 4 carbon atoms, and their use as intermediates in the preparation of antibacterial 2,4-diamino-5-benzylpyrimidines. They are prepared from a reaction between an orthoester and an .alpha.-substituted-.beta.-benzylpropionitrile and then the resulting cyanoacetal is converted to the benzyl-pyrimidine by reaction with guanidine.
Claims14
A benzyl cyanoacetal of formula (I), ##STR10## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is a halogen or hydrogen atom, an alkoxy group, an alkyl group or a dialkylamino group;
- R.sup.4 is an alkoxy carbonyl group or an aldehyde group;
- and R.sup.5 is an alkyl group;
- the alkyl or alkoxy groups each having from 1 to 4 carbon atoms.
.alpha.-Dimethoxymethyl-.alpha.-formyl-.beta.-(3,4,5-trimethoxyphenyl) propionitrile.
.alpha.-Diethoxymethyl-.alpha.-formyl-.beta.-(3,4,5-trimethoxyphenyl) propionitrile.
.alpha.-Car bothoxy-.alpha.-diethoxymethyl-.beta.-(3,4,5-trimethoxyphenyl) propionitrile.
Dependencies are inferred from the claim text.