Alternative synthesis of renin inhibitors and intermediates...

Details Alternative synthesis of renin inhibitors and intermediates... Alternative synthesis of renin inhibitors and intermediates...

2011-03-22

2011-03-22

Kumar, Shailendra (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

Reexamination Certificate

active

07910774

ABSTRACT:
The present invention relates to synthetic routes to prepare a compound of the formulawherein R1is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2is halogen, C1-4alkyl or C1-4alkoxy; R3and R4are independently branched C3-6alkyl; and R5is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

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Göschke et al., Helvetica Chimica Acta, vol. 86, pp. 2848-2870, “The nonchiral bislactim diethoxy ether as a highly stereo-inducing synthon for sterically hindered, γ-branched α-amino acids: a practical, large-scale route to an intermediate of the novel renin inhibitor aliskiren”, (2003).
Hanessian et al., J. Org. Chem., 67, pp. 4261-4274, “The power of visual imagery in synthesis planning, stereocontrolled approaches to CGP-60536B, a potent renin inhibitor”, (2002).G.
Rueger et al., Tetrahedron Letters 41, pp. 10085-10089, A convergent synthesis approach towards CGP60536B, a non-peptide orally potent rennin inhibitor, via an enantiomerically pure ketolactone intermediate ,(2000).
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