On May 20, 2010, Soll, Mark David; Le Hir De Fallois, Loiec Patrick; Huber, Scot Kevin; Lee, Hyoung Ik; Wilkinson, Douglas Edward; Jacobs, Robert Toms; Beck, Brent Christopher published a patent.Synthetic Route of 1086838-13-2 The title of the patent was Preparation of enantiomerically enriched aryloazol-2-yl cyanoethylamino parasiticidal compounds. And the patent contained the following:
The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula I (wherein P is C-R1 or N; Q is C-R2 or N; V is C-R8 or N; W is C-R9 or N; X is C-R10 or N; Y is C-R11 or N; R1, R2 R8, R9, R10 and R11 are independently H, NH2, amido, etc.; R3, R4 and R5 are independently H, halo, alkyl, etc., or R4 and R5 form part of a cycloalkyl ring; R6 is H, alkyl, alkoxyalkyl, etc. ; R7 is H, alkyl, cycloalkyl, etc.; Z is a direct bond, C(O), C(S) or S(O)p; a = 1-3; p = 0-2), compositions thereof, processes for their preparation, and their uses as pesticides, in particular for controlling endo- and ectoparasites that are harmful to mammals, fish and birds. Example compound II, prepared by reacting 4-trifluoromethoxybenzoyl chloride and (R)-2-amino-3-(6-bromopyrazolo[4,3-b]pyridin-2-yl)-2-methylpropionitrile (preparation given), showed 100% efficacy against ivermectin-resistant endoparasites at an oral dose of 1.5 mg/kg in sheep. The experimental process involved the reaction of 5-Chloro-3-nitropicolinaldehyde(cas: 1086838-13-2).Synthetic Route of 1086838-13-2
The Article related to enantiomerically enriched aryloazolyl cyanoethylamino parasiticide preparation, benzotriazole cyanoethylamino preparation antiparasitic endoparasite ectoparasite, indazole cyanoethylamino preparation parasiticidal infection, endoparasite ectoparasite pesticidal pyrazolopyridine cyanoethylamino preparation and other aspects.Synthetic Route of 1086838-13-2