Pharmaceuticals antihypertensive

Diuretics. The diuretic and antihypertensive agent bendrodumethia2ide [73 8-3] is a ben2otriduoride-based pharmaceutical. 

Cyclothia2ide [2259-96-3] is another example of a duorine-free pharmaceutical (diuretic, antihypertensive) based on y -chloroduoroben2ene [625-98-9] where duorine activation is subsequentiy provided by two sulfonamide groups (156). 

Another important reaction of diketene derivatives is the Hant2sch pyridine synthesis (101). This synthesis is the preparation of 1,4-dihydropyridines (14) starting either from two acetoacetic esters, which react with an aldehyde and ammonia or a primary amine or from 3-aminocrotonates and 2-alkyhdene acetoacetic esters, both diketene derivatives. Several such dihydropyridines such as nifedipine [21829-25-4] (102), nimodipine [66085-59-4] and nicardipine [55985-32-5] exhibit interesting pharmaceutical activity as vasodilators (blood vessel dilation) and antihypertensives (see Cardiovascularagents). 

Pharmaceutical Products. Rhc ne-Poulenc offers a flaked technical-grade vanillin, Vaniltek, to be used in pharmaceutical appHcations. The single largest use for vanillin is as a starting material for the manufacture of an antihypertensive dmg having the chemical name of Methyldopa or L-3-(3,4-dihydroxyphenyl)-2-methylalanine. 

Side chain reaction in derivatives of compound 2 has largely been concerned with the production of compounds with pharmaceutical activity by reaction between chloroalkyl side chains in position 2 and suitable amines. A selection of such compounds are 224 (82JAP(K)206684), and 225 (81FRP2450259) both are antihypertensive. Use of a dichloromethyl side chain provides an unsaturated amine, as in compound 226 (81FRP2450259). 

Many alkaloids have pronounced biological properties, and a substantial number of the pharmaceutical agents used today are derived from naturally occurring amines. As a few examples, morphine, an analgesic agent, is obtained from the opium poppy Papaver somnifemm. Cocaine, both an anesthetic and a central nervous system stimulant, is obtained front the coca bush Erythroxylon coca, endemic to upland rain forest areas of Colombia, Ecuador, Peru, Bolivia, and western Brazil. Reserpine, a tranquilizer and antihypertensive, comes from powdered roots of the semitropical plant Rauwolfia serpentina. Ephedrine, a bronchodilator and decongestant, is obtained front the Chinese plant Ephedra sinica. 

Immaculada Rapado-Martinez, M., Garcia-Alvarez-Coque, C., and Villanue-va-Camanas, R.M., Performance of micellar mobile phase in reversed-phase chromatography for the analysis of pharmaceuticals containing [i-blockers and other antihypertensive drugs, Analyst, 121,1677, 1996. 

Apart from pharmaceuticals, peptides are also used for diagnostics and vaccines. More than 40 peptides are in commercial use today. A dozen of them is shown in Table 3.1. As shown in column 3 of the table, the number of amino acids that make up a specihc peptide varies widely. At the low end there are dipeptides, like the blockbuster antihypertensive drug enalapril and the artihcial sweetener Aspartame (not shown in the table). In terms of volumes produced, there are by far the most important product group. At the high end there is the anticoagulant Hirudin, which is composed of 65 amino acids. Sales of synthetic peptides are estimated at 4 billion as formulated drugs (resp. 300- 400 million as APIs). 

Powers, R. L., K. A. Halbritter, J. G. Arbogast, J. L. Neely, and A. J. Williams. 1998. Do Interactions with Pharmaceutical Representatives Influence Antihypertensive Medication Prescribing Practices of Family Medicine and General Internal Medicine Physicians Journal of General Internal Medicine 13, Supplement 13. 

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