37845-05-9Relevant articles and documents
Preparation process of amantadine nitrate derivative
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, (2019/01/24)
The invention discloses a preparation process of an amantadine nitrate derivative, and the amantadine nitrate derivative is prepared from substituted or unsubstituted adamantane as a raw material by the following steps: (1) synthesizing of adamantanol; (2) carboxylation of the adamantanol; (3) amidation of adamantane acid; (4) reduction; (5) hydrolysis of acylamino adamantanol and boc protection of amino; (6) crystallization of Boc-protected amantadine alcohol; (7) nitric acid esterification of Boc-protected amantadine alcohol; (8) refining of a nitric acid esterification product; (9) amino deprotection and salt formation; and (10) refinement of amantadine nitrate. The amantadine amine nitrate derivative is as shown in the specification, wherein R1 and R2 are same or different, and are respectively hydrogen, a linear or branched alkyl group, a substituted or unsubstituted aryl group and a hetero aryl group. The preparation process is efficient, economic, green, safe and reliable and issuitable for industrial production.