主权项 |
1. Method for synthesizing a compound of Formula (II)wherein
R1 is a nitrogen-protecting group derivable from an amino group selected from the group consisting of tosylamide (Ts), t-butyl carbamate (Boc), benzyl carbamate (Cbz), 9-fluorenylmethyl carbamate (Fmoc), acetamide (Ac), trifluoroacetamide (TFA), benzylideneamine, triphenylmethylamine (Tritylamine), benzylamine (Bn), and phthalimide; R2 is selected from the group consisting of halogen, —C(O)—R, —NRR′, —OR, —SR, —COOR, —CN, —NO2, —C(O)—NRR′, —NR′—C(O)—R, —SO2—R, —(SO2)—OR, linear or branched, substituted or unsubstituted C1-C10 alkyl; linear or branched, substituted or unsubstituted C2-C10 alkenyl; linear or branched, substituted or unsubstituted C2-C10 alkynyl; linear or branched, substituted or unsubstituted C1-C10 alkoxy; substituted or unsubstituted C3-C10 cycloalkyl; substituted or unsubstituted C3-C10 cycloalkenyl; substituted or unsubstituted C6-C10 aryl; substituted or unsubstituted C3-C10 heteroaryl; R and R′ are independently selected from the group consisting of H and linear or branched, substituted or unsubstituted C1-C10 alkyl;the method comprising:
reacting a compound of Formula (I) with NH2R1 to form a compound of Formula (IV) reacting the compound of Formula (IV) with a precursor of R2 in the presence of a rhodium catalyst to form an enantiomer of a compound of Formula (V) reacting the compound of Formula (V) with an oxidizing agent to form a compound of Formula (VI) reacting the compound of Formula (VI) with a reducing agent to form a compound of Formula (VII) hydrogenating the compound of Formula (VII) to form the compound of Formula (II). |