Industrial chemistry in the new millennium is widely adopting the con-cept of “Green chemistry” to meet the fundamental scientific challenges. Antihy-pertensive drugs include several of the most widely prescribed drugs like diuretics, beta-blockers, ACE inhibitors, calcium channel blockers, and α-1 adrenorecep-tor blockers. The discovery of prazosin, with very high index of α1/α2 affinity has triggered off a renaissance of interest in αα1-adrenoceptor antagonist drugs for treat-ment of hypertension. The three reported routes for synthesis and manufacture of the α-adrenoceptor antagonist- prazosin had some disadvantages. In present study we had developed new methods for the synthesis of prazosin by using microwave. The most important aspect is the overall yield of this process was ~25 % higher than the other reported methods excluding the use of banned substances.