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Amino-oxides and halomethyl organometallic reagent formed in situ.

机译:氨基氧化物和卤甲基有机金属试剂原位形成。

摘要

Invention Patent: "AMINO-POXIDES OF ENVIROLDED AND ORGANOMETAL REAGENT FORMED IN SITU". Method for the preparation of an amino oxide where a protected amino-oxide is reacted with an orgamethalic halomethyl reagent in a solvent appropriate at a temperature above 80th C where the said organometallic reagent is formed by the reaction between an organometallic reagent and a dihalomethane, the improvement comprising the flow of protected aminoaldehyde into a mixing zone maintained at a temperature below 0.C,Also flowing the said organometallic halomethyl reagent in the said contact mixing zone in the said blending zone with the protected aminoaldehyde and also removing products from the said aminoaldehyde mixing zone and said organometallic halomethyl reagent. The aminoaldehydes obtained are useful through the opening of amine of the Epoxide ring as intermediaries in the preparation of pharmaceutical products, e.g. HIV protease inhibitors.
机译:发明专利:“原位制成的被包封的有机试剂的氨基氧化物”。制备氨基氧化物的方法,其中将受保护的氨基氧化物与邻氨基苯甲酸酯卤代甲基试剂在适当的溶剂中,在高于80°C的温度下反应,其中所述有机金属试剂是通过有机金属试剂与二卤甲烷之间的反应形成的,改进包括使受保护的氨基醛流入保持在低于0℃的温度的混合区中,还使所述有机金属卤代甲基试剂在所述混合区中的所述接触混合区中与受保护的氨基醛一起流动,并且还从所述氨基醛中除去产物混合区和所述有机金属卤代甲基试剂。所获得的氨基醛可通过环氧化物的胺的开环作为中间体,用于制备药物产品,例如苯酚。 HIV蛋白酶抑制剂。

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