5331. Lacidipine

Nomenclature

CAS number: 103890-78-4
(E)-4-[2-[3-(1,1-Dimethylethoxy)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid diethyl ester; diethyl (E)-4-[2-[2-(tert-butoxycarbonyl)vinyl]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate; 4-[o-[(E)-2-carboxyvinyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid 4-tert-butyl diethyl ester; GR-43659X; GX-1048; Caldine (Boehringer, Ing.); Lacimen (Menarini); Lacipil (GSK); Lacirex (Guidotti); Midotens (Boehringer, Ing.); Motens (Boehringer, Ing.).
C26H33NO6; mol wt 455.54.
C 68.55%, H 7.30%, N 3.07%, O 21.07%.

Description and references

Dihydropyridine calcium channel blocker. Prepn: C. Semeraro et al., DE 3529997; eidem, US 4801599 (1986, 1989 both to Glaxo). Clinical pharmacology: M. Safar et al., Clin. Pharmacol. Ther. 46, 94 (1989). HPTLC determn in urine: V. R. Kharat et al., J. Pharm. Biomed. Anal. 28, 789 (2002). Clinical trial in atherosclerosis: A. Zanchetti et al., Circulation 106, 2422 (2002). Review of use in hypertension: P. L. McCormack, A. J. Wagstaff, Drugs 63, 2327-2356 (2003).

Chemical structure

Properties

Crystalline solid from ethyl acetate, mp 174-175°.

Therapeutic Category

Antihypertensive.

Keywords

Antihypertensive; Dihydropyridine Derivatives; Calcium Channel Blocker; Dihydropyridine Derivatives