Process for preparing d,1-m,p-dipivalylepinephrine...

C - Chemistry – Metallurgy – 07 – D

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260/472, 260/479

C07D 213/79 (2006.01) A61K 31/135 (2006.01) A61K 31/24 (2006.01) B01J 23/42 (2006.01) C07C 67/14 (2006.01) C07D 213/55 (2006.01) C07D 213/81 (2006.01) C07D 213/82 (2006.01)

Patent

CA 1102336

ABSTRACT OF THE DISCLOSURE Compounds of the formula Image wherein R represents a straight or branched C1-C5 alkyl group; and R1 in each occurrence represents an acyl member which is alkanoyl having 1-22 carbon atoms, alkenoyl having one or two double bonds and having 4-22 carbon atoms, cycloalkyl-CnH2n-?- having a total of 4-10 carbon atoms of which 3-7 are ring carbon atoms in cycloalkyl and wherein n is zero, one, or two,phenoxy- acetyl, naphthalenecarbonyl, pyridinecar??nyl, phenyl-CnH2n-?- wherein n is zero, one or two and phenyl is unsubstituted or is substituted by 1-3 alkyl having 1-4 carbon atoms, alkoxy having 1-4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2-8 carbon atoms, or alkanoylamino having 1-6 carbon atoms groups; are prepared in substantial purity and yield, using as the chloride ion donor, cesium chloride (CsCl). The compounds prepared by the process claimed herein exhibit sympathomimetic activity and are thus useful in elicit- ing sympathomimetic responses in warm-blooded animals, e.g., reduction in intraocular pressure, miosis, mydriasis, broncho- dilation, etc.

282259

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