Captopril is an antihypertensive agent that inhibits the angiotensin-converting enzyme of the renin-angiotensin system. Chiral intermediates are used in the synthesis of the drug. These intermediates are obtained by resolution of racemic compounds or by chemical, biocatalytic methods and or by asymmetric synthesis by biocatalytic process. This article reviews the various chemical and biochemical processes involved in the synthesis of the chiral drug, including the pharmacological action of captopril.