摘要 |
<p>N-Aryl-2,2-dihalo-acetamidine derivs. of formula (I): (where R1, R2 and R3 are H, halogen, an aliphatic residue, or a group OR4 (R4=aliphatic or aromatic residue); and X is halogen) are prepd. by a new process in which a trihalo-acetaldehyde animal deriv. of formula (II) (where R5 is H, alkoxy, or an aliphatic or aromatic residue) is reacted with at least one molar equivalent of a basic alkali(ne earth) cpd. and/or a tertiary amine. Cpds. (I) in which R1, R2 and R3 are other than H are claimed as new cpds. (I) are useful as pesticides (esp. fungicides) and pharmaceuticals. They are also useful as intermediates for pesticides (esp. fungicides), pharmaceuticals and dyes. The new process is simpler and more economical than known processes, and gives (I) in improved yields and purity. Specific cpds. (I) include 2,2-dichloro-N-(3,4-dichlorophenyl)-acetamidine. In an example, this is prepd. in 75% yield by slowly treating a solution of N-(3,4-dichlorophenyl)-N'-formyl-3,3,3-trichloroacetaldehyde aminal (33.7g) in 95% EtOH (150ml) with NaOH (8g) in EtOH (80ml) and stirring 12 hrs.</p> |