New bestatin derivs. are cpds. of formula R1CH(NH2).CH(OH).CO.NH.CH(R2).COOH (I), where R1 is hydroxybenzyl; and R2 is 1-6C alkyl, hydroxyalkyl, mercaptoalkyl, carboxamidoalkyl, alkoxyalkyl, alkylmercaptoalkyl, carboxyalkyl, aryl, aralkyl or substd. aralkyl. Specific cpds. (I) include (2RS, 3RS)-3-amino-2-hydroxy-4-(p-hydroxyphenyl)-butyryl-(5)-leucine. In an example, this is prepd. by (a) refluxing Z-(2RS, 3RS)-3-amino-2-hydroxy-4-(p-methoxyphenyl)butyronitrile with conc. HCl and dioxan in the presence of anisole; (b) reacting the resulting (2RS, 3RS)-3-amino-2-hydroxy-4-(p-hydroxyphenyl)butyric acid with Z-Cl in the presence of NaOH; (c) reacting the resulting Z-(2RS, 3RS)-3-amino-2-hydroxy-4-(p-OZ-phenyl)butyric acid with Leu-OB3I in the presence of N-hydroxybenzotriazole; and (d) hydrogenating the resulting Z-(2RS, 3RS)-3-amino-2-hydroxy-4-(p-OZ-phenyl)-butyryl-(5)-leucine benzyl ester over palladium black.
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机译：新的Bestatin衍生。是cpds。式R1CH（NH2）.CH（OH）.CO.NH.CH（R2）.COOH（I）的化合物，其中R1是羟基苄基; R 2是1-6C烷基，羟基烷基，巯基烷基，羧酰胺基烷基，烷氧基烷基，烷基巯基烷基，羧基烷基，芳基，芳烷基或亚甲基。芳烷基。特定的cpds。 （I）包括（2RS，3RS）-3-氨基-2-羟基-4-（对羟基苯基）-丁酰基-（5）-亮氨酸。在一个示例中，这是准备的。通过（a）将Z-（2RS，3RS）-3-氨基-2-羟基-4-（对甲氧基苯基）丁腈与浓溶液回流。苯甲醚存在下的HCl和二恶烷; （b）在NaOH存在下使所得的（2RS，3RS）-3-氨基-2-羟基-4-（对羟基苯基）丁酸与Z-Cl反应; （c）在N-羟基苯并三唑存在下，使所得的Z-（2RS，3RS）-3-氨基-2-羟基-4-（对-OZ-苯基）丁酸与Leu-OB3I反应; （d）在钯黑上氢化所得的Z-（2RS，3RS）-3-氨基-2-羟基-4-（对-OZ-苯基）-丁酰基-（5）-亮氨酸苄酯。
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