C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/235.95, 260/
C07D 251/08 (2006.01) A01N 43/64 (2006.01) A01N 47/12 (2006.01) A01N 47/18 (2006.01) A01N 47/20 (2006.01)
Patent
CA 1110622
Abstract The prevention of ticks in the raising of domestic animals is of concern particularly with regard to weight gain and meat quality in agricul- tural animals. There is always a need for novel ectoparasiticidal agents. The present invention meets this need by providing a process for preparing a compound of the formula: Image (I) wherein R is an alkyl, cycloalkyl, adamantyl, lower alkenyl, or a lower- alkynyl group or d substituted-lower alkyl group wherein the substituent is a hydroxy, lower alkoxy, lower alkanoyloxy, carbamoyloxy, N-lower alkyl- carbamoyloxy, N-cycloalkyl-carbamoyloxy, N-aryl-carbamoyloxy, thiocarbamoyloxy, N-lower alkyl-thiocarbamoyloxy, N-cycloalkyl-thiocarbamoyloxy, N-aryl- thiocarbamoyloxy, aryl-sulphonyloxy, mono- or di-lower alkyl-amino or an aryl group; R1 is a lower alkyl or hydroxy-methyl group; and X is a hydrogen atom or a lower alkyl group; and pharmaceutically acceptable acid addition salts thereof; which comprises (a) reacting a thiourea of the formula: Image (II) wherein R2 is hydrogen or lower alkyl and X is a previously defined; with an amine of tho formula RNH2, where R is as previously defined, in the presence of formaldehyde: (b) acylating sulphonylating, or reacting with potassium isocyanato or isothiocyanate or with a lower alkyl, cycloalkyl or an aryl isocyanato or isothiocyanate, a compound of formula I as defined above wherein R is a hydroxy-lower alkyl group; and (c) reacting a compound of formula I as defined above wherein R2 is hydrogen with formaldehyde; and where required forming a pharmaceutically acceptable acid addition salt of the resulting product.
307810
Leeming Michael R.g.
Narayanaswami Subramaniyan
Penrose Alexander B.
Pfizer Corporation
Smart & Biggar
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