Patent ID: 6022996
Filing Date: 2000-02-08
Classification: A61K,C07B,C07C,C07D,C07K

Abstract:
A method of forming a protected alpha-aminoaldehyde of Formula III: ##STR9## wherein P.sup.1 and P.sup.2 independently are selected from the group consisting of acyl, aralkyl, alkenyl, silyl, aralkoxycarbonyl and cycloalkenylalkyl radical amine protecting groups;wherein further P.sup.1 and P.sup.2 may be taken together with the nitrogen atom of Formula II to form a heterocyclic ring system containing said nitrogen atom as a ring member;wherein R.sup.1 is selected from the group consisting of alkyl, aryl, cycloalkyl, cycloalkylalkyl and aralkyl, which are optionally substituted with a member selected from the group consisting to alkyl, halo, NO.sub.2, OR.sup.9, and SR.sup.9, wherein R.sup.9 is selected from the group consisting of hydrogen and alkyl;and wherein any of the foregoing groups of P.sup.1, P.sup.2 and R.sup.1 may be substituted at one or more substitutable positions with one or more radicals independently selected from the group consisting of halo, alkyl of C.sub.1 -C.sub.8, alkoxy, hydroxy, nitro, alkenyl, amino, alkylarnino, acylamino, acyl and a pharmaceutically-acceptable salt thereof;said method comprising treating at a temperature of about 0.degree. C. to about 30.degree. C. a protected amino alcohol of the following formula; ##STR10## with an oxidizing agent.