- Practical asymmetric synthesis of a chiral piperazinone derivative
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A practical asymmetric route to a chiral piperazinone derivative, a fragment of MK-3207, is reported. The amine-bearing benzylic stereocenter is introduced via an asymmetric Pd-catalyzed hydrogenation of a cyclic sulfimidate in the presence of a chiral phosphine ligand. An efficient synthesis of the hydrogenation substrate is described, together with process development of the hydrogenation step and elaboration of the resulting cyclic sulfamate product to the desired piperazinone.
- McLaughlin, Mark,Belyk, Kevin,Chen, Cheng-Yi,Linghu, Xin,Pan, Jun,Qian, Gang,Reamer, Robert A.,Xu, Yingju
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p. 1052 - 1060
(2013/09/12)
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- Substituted monocyclic CGRP receptor antagonists
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Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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Page/Page column 53
(2008/06/13)
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