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    • 5. 发明授权
    • Synthesis of dl-2-amino-1-butanol
    • dl-2-氨基-1-丁醇的合成
    • US3944617A
    • 1976-03-16
    • US493801
    • 1974-08-01
    • Balwant Singh
    • Balwant Singh
    • C07C89/00C07C91/04
    • C07C231/10C07C233/13C07C249/02C07C257/02C07B2200/07Y02P20/582
    • DL-2-Amino-1-butanol, as the free base or a salt, for resolution to d-2-amino-1-butanol, for the synthesis of ethambutol hydrochloride, d,d'-2,2'-(ethylenediimino)di-1-butanol dihydrochloride, is produced in high purity and good yields by the reaction of butene-1, a nitrile, preferably an excess of acetonitrile, and chlorine to form N-[1-(chloromethyl)propyl]acetimidoyl chloride which is hydrolyzed to dl-2-amino-1-butanol hydrochloride. This can be isolated as the hydrochloride, or free base, or a mixture, resolved with L(+)- tartaric acid and the d-2-amino-1-butanol reacted with ethylene dichloride and then hydrochloric acid to form ethambutol hydrochloride. A minimum of by-products which are conveniently split out permits the economical synthesis of a pharmaceutical grade product.
    • 作为游离碱或盐的DL-2-氨基-1-丁醇,用于分解为d-2-氨基-1-丁醇,用于合成乙胺丁醇盐酸盐,d,d'-2,2' - (亚乙基二亚氨基 )二-1-丁醇二盐酸盐通过丁烯-1,腈,优选过量的乙腈和氯反应生成高纯度和良好的产率,以形成N- [1-(氯甲基)丙基]亚氨代乙酰氯,其中 被水解成dl-2-氨基-1-丁醇盐酸盐。 这可以用盐酸盐或游离碱或混合物分离,用L(+) - 酒石酸和d-2-氨基-1-丁醇与二氯乙烷反应,然后与盐酸反应形成乙胺丁醇盐酸盐。 方便分开的最少副产物允许经济地合成药物级产品。
    • 10. 发明授权
    • Synthesis of ethambutol
    • 乙胺丁醇的合成
    • US3944618A
    • 1976-03-16
    • US493802
    • 1974-08-01
    • Balwant Singh
    • Balwant Singh
    • C07C89/00C07C89/04C07C91/04
    • C07C231/10C07C233/13C07C249/02C07C257/02C07B2200/07Y02P20/582
    • D-2-Amino-1-butanol, for the synthesis of ethambutol hydrochloride, d,d'-2,2'-(ethylenediimino)di-1-butanol dihydrochloride, is produced in high purity and good yields by the reaction of butene-1, a nitrile, preferably an excess of acetonitrile, and chlorine to form N-[1-(chloromethyl)propyl]acetimidoyl chloride which is hydrolyzed to dl-2-amino-1-butanol, which can be isolated as the hydrochloride, or free base, or a mixture, resolved with L(+)-tartaric acid and the d-2-amino-1-butanol reacted with ethylene dichloride and then hydrochloric acid to form ethambutol hydrochloride. A minimum of by-products which are conveniently split out permits the economical synthesis of a pharmaceutical grade product.
    • 用于合成乙胺丁醇盐酸盐d,d'-2,2' - (乙二胺基)二-1-丁醇二盐酸盐的D-2-氨基-1-丁醇通过丁烯反应以高纯度和良好的收率生产 -1,腈,优选过量的乙腈和氯,以形成水解成dl-2-氨基-1-丁醇的N- [1-(氯甲基)丙基]亚氨代乙酰氯,其可以作为盐酸盐分离, 或游离碱或混合物,用L(+) - 酒石酸和d-2-氨基-1-丁醇分解,与二氯乙烷反应,然后与盐酸反应,形成乙胺丁醇盐酸盐。 方便分开的最少副产物允许经济地合成药物级产品。