Steroidal isoxazolines

Zoetis launches Simparica, a new chewable monthly flea and tick preventative (March 2016)
Simparica (sarolaner) Chewables received European Commission endorsement in November as an approved killer of four common European ticks and two types of fleas. The . formulation is indicated for use against adult fleas, flea infestations and the Lone Star, Gulf Coast, American and brown dog ticks. Sarolaner, the active ingredient in Simparica, is in the same isoxazoline class as Bravecto and NexGard (see below). The company claims that its product kills fleas faster than NexGard, preventing them from reproducing. Each tablet is effective for one month. They are approved for dogs at least six months in age.
Update: A new study shows that Simparica at the usual flea-preventive dose is effective against demodectic mange (demodex), as well as otodectic mange. See Demodex below for more information.

A solution of 21 (acetyloxy) 9 fluoro 11/p hydroxy 16 methyl 10 pregna 1,4,16 triene 3,20 dione ( 100 mg) and a ethoxycarbonyl N methyl nitrone ( 152 mg) in dry toluene ( 6 0 ml) is refluxed under an atmosphere of nitrogen for 48 hours The mixture is then cooled, diluted with chloroform, washed successively with 5 %o hydrochloric acid, a dilute sodium bicarbonate solution and water, dried and evaporated to a residue From this the title compound is isolated 15 by preparative thin layer chromatography (silica gel plates; developed with chloroform-methanol, 97:3) One crystallization from ethyl acetate-hexane affords 57 mg of material, melting point 241-242 C (dec) (discoloration starts from 232 C).

Steroidal isoxazolines

steroidal isoxazolines

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