[35] Solid Phase Synthesis of Luteinizing Hormone-Releasing Hormone and Its Analogues

The elucidation of the structure of luteinizing hormone–releasing hormone (LH-RH) (II), isolated from both porcine and ovine hypothalami led rapidly to the synthesis of the decapeptide by both classic and solid phase techniques. The natural and synthetic materials also stimulate the release of follicle stimulating hormone (FSH) in animals and human beings. There is considerable interest in establishing structure-activity relationships for this decapeptide and particularly in finding related compounds that might inhibit, instead of stimulate, the release of LH and FSH from the pituitary. This would aid in developing new methods for birth control using antagonistic analogues of LH-RH. The demand for large amounts of pure synthetic LH-RH for extensive studies in laboratory and domestic animals and human beings has resulted in the development in this laboratory of a convenient and reliable synthesis of the hormone by the use of the Merrifield solid phase method. This method has also been utilized with success to synthesize analogues of LH-RH.