Generation of synthetic equivalents of RCH(Li)NH2 for the synthesis of primary amines. Tin-lithium exchange on carbamate-protected (.alpha.-aminoalkyl)stannanes
ecologically safer way to synthesize protected amines, the reactions of amines with benzyl halides under CO2 atmosphere were systematically examined. For primary amines, the CO2-inserted products were obtained in higher yields in the presence of DBU as a base, under a high pressure of CO2, and in a low-polarity solvent (toluene/hexane 1 : 1). Secondary amines gave only low yields of CO2-inserted products
为了找到一种有用、实用且生态更安全的合成受保护胺的方法,系统地研究了胺与卤代苄在 CO2 气氛下的反应。对于伯胺,在 DBU 作为碱的存在下,在 的高压下,在低极性溶剂(甲苯/己烷 1:1)中,以更高的产率获得了插入 的产物。仲胺仅产生低产率的 插入产物。
[EN] BIS-AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS<br/>[FR] HYDROXYETHYLAMINO SULFONAMIDE DE BIS-AMINOACIDE INHIBITEURS DE PROTEASES DE RETROVIRUS
申请人:G.D. SEARLE & CO.
公开号:WO1996028464A1
公开(公告)日:1996-09-19
(EN) Selected bis-amino acid hydroxyethylamino sulfonamide compounds of formula (I) are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and the treatment of a retroviral infection.(FR) L'invention porte sur une sélection de composés du type hydroxyéthylamino sulfonamide de bis aminoacide de formule (I) s'avérant efficaces comme inhibiteurs de protéases rétrovirales et notamment de celle du VIH, sur lesdits inhibiteurs de protéases rétrovirales, et plus particulièrement sur de nouveaux composés sélectionnés, une composition et un procédé d'inhibition des protéases rétrovirales telle que celle du VIH humain, de prévention prophylactique et de traitement des infections rétrovirales, et de prévention de la dissémination d'un rétrovirus.