- A Concise Stereoselective Synthesis of (R)-2-Benzylmorpholine and ML398 from (R)-(?)-2-Phenylglycinol
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We describe here an efficient stereoselective method for the preparation of (R)-2-benzylmorpholine and ML398. The present method features a high diastereocontrol using an endocyclic oxidation of phenylglycinol-derived morpholine and a stereoselective alky
- Torres, Saúl,Velasco, Manuel,Gallegos-Rojas, José ángel,Bernès, Sylvain,Orea, María L.,Terán, Joel L.,Huelgas, Gabriela,Gómez-Calvario, Víctor,Juárez, Jorge R.
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p. 2677 - 2682
(2019/08/21)
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- AZAQUINAZOLINE INHIBITORS OF ATYPICAL PROTEIN KINASE C
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The present invention provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.
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- COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein, R1, R2, A, Y, X, Ar1 and Ar2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.
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Page/Page column 49-50
(2008/06/13)
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- Binding of 2,4-substituted morpholines at human D4 dopamine receptors
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The synthesis of a series of 2,4-disubstituted morpholines is described and their affinities at human dopamine receptors reported. The orally bioavailable 7-azaindole compound 11 has nanomolar affinity at the hD4 receptor with > 1000-fold selectivity over the hD2 receptor.
- Showell, Graham A.,Emms, Frances,Marwood, Rosemarie,O'Connor, Desmond,Patel, Smita,Leeson, Paul D.
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- Synthesis and resolution of the novel appetite suppressant 2-benzylmorpholine, a nonstimulant isomer of phenmetrazine
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The synthesis of 2-benzylmorpholine from allylbenzene together with its resolution into its (+)- and (-)-enantiomers is reported. Oral dosing of the racemate to dogs caused appetite suppression with an ED50 of 3 and 5.5 mg kg-1 at 1 and 2 h, re
- Brown,Forster,Foubister,Stribling
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p. 797 - 799
(2007/10/02)
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