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US 2011/0034446 A1Published application
R(-)-2-methoxy-11-hydroxyaporphine and derivatives thereof
AssigneeThe McLean Hospital Corporation
InventorsJohn L. Neumeyer, Yu-Gui Si
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Abstract
The invention features derivatives of R(−)-2-methoxy-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.
Claims21
A compound of formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein
- Y1 is H, C(O)—R3, C(O)—O—R3, C(O)—NR3R4, P(O)(OH)—O—R3, C(S)—R3, C(S)—O—R3, C(S)—NR3R4, or fatty acid acyl;
- R1 is H, C1-4 alkyl, C2-4 alkenyl, or C2-4 alkynyl;
- and
- each of R3 and R4 is, independently, selected from H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C2-6 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-7 heteroalkyl, or R3 and R4 together form a heterocyclic ring containing at least one nitrogen atom.
3 more elements
A method for synthesizing a compound of formula III from a compound of formula III:
- said method comprising the step of reducing said compound of formula II with magnesium metal in methanol in the presence of Pd/C catalyst, wherein
- P1 is H, or a hydroxyl protecting group other than CH3SO2— or CF3SO2—;
- X2 is CH3SO2— or CF3SO2—;
- and
- R1 is H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, or an amine protecting group.
2 more elements
Dependencies are inferred from the claim text.