【摘要】 4-氮杂类甾体化合物是一类比较重要的治疗良性前列腺增生、男性秃顶、女性多毛等症状的5α还原酶抑制剂.以4雄烯二酮为起始原料,经过氧化开环、氨解闭环、肟化、取代等4-步反应,合成了3个新的3-羰基-4-氮杂-5-雄甾烯-17肟衍生物7、8和9,并用质谱、1HNMR、13CNMR等测试手段对目标化合物的结构进行了表征.更多还原

【Abstract】 4-Azasteroids as important 5α-reductase inhibitors play a critical role in therapy of several human endocrine diseases, such as benign prostatic hyperplasia, male pattern baldness, female hirsutism, etc. Starting from 4-androstenedione, three novel 3-oxo-4-aza-5-androstene-17-oxime derivatives 7, 8 and 9 were synthesized through oxidation ring cleavage, amination ring closure, oximation,and substitution. The structures of these novel compounds were identified with MS, 1H NMR and 13C NMR.更多还原