73644-95-8Relevant academic research and scientific papers
SUBSTITUTED PROLINAMIDES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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Page/Page column 15, (2009/03/07)
The present invention provides new substituted prolinamides of the general formula (I) in which D, L, E, G, J, M, R3, R4, R5, and R13 are defined as in claim 1, their tautomers, their enantiomers, their diastere
Classical and dynamic resolution of 1-amino-3-methyl-1,3,4,5- tetrahydrobenzo[d]azepin-2-one
Mitchell, David,Hay, Lynne A.,Koenig, Thomas M.,McDaniel, Stacey,Nissen, Jeffrey S.,Audia, James E.
, p. 3814 - 3819 (2007/10/03)
Two efficient production processes of enantioenriched 1-amino-3-methyl-1,3, 4,5-tetrahydro-benzo[d]azepin-2-one 1 were achieved using the readily available starting materials. A key step in the methodologies is a classical resolution or a dynamic resolution that provides excellent chemical (>80%) yields and enantiomeric excesses (>99.8% ee). The classical resolution was developed on a preparative scale while the dynamic resolution was implemented on a pilot plant scale.
SYNTHESIS OF 5-HYDROXY-3-TRIFLUOROMETHYL-PYRAZOLES BY RING OPENING OF 3-TRIFLUOROACETYL-BENZOLACTAMS
Bouillon, J.P.,Janousek, Z.,Viehe, H. G.,Tinant, B.,Declercq, J.P.
, p. 655 - 664 (2007/10/02)
New trifluoromethylated pyrazoles 5b,c,f have been prepared by condensation of 3-trifluoroacetyl benzolactams 1a,b,c and 2 with hydrazines by opening of the lactam moiety.The structure of pyrazoles was established by X-ray diffraction analysis and by comp
ACID-CATALYZED CYCLIZATIONS OF AROMATIC DIAZOACETAMIDES: SYNTHESIS OF SPIRODIENONE LACTAMS, ISOQUINOLINES, AND BENZAZEPINONES
Rishton, Gilbert M.,Schwartz, Martin A.
, p. 2643 - 2646 (2007/10/02)
Acid-catalyzed cyclizations of aromatic diazoacetamides produce good yields of simple isoquinolinones and benzazepinones.The intermediacy of spirodienone oxonium species has been demonstrated by trapping and isolation of synthetically useful spirodienone
BENZOLACTAMS-1. ALKYLATION OF 1,2,4,5-TETRAHYDRO-3-METHYL-3H-3-BENZAZEPIN-2-ONE WITH SODIUM HYDRIDE AND ALKYL HALIDE
Orito, Kazuhiko,Matsuzaki, Tsutomu
, p. 1017 - 1021 (2007/10/02)
Alkylation of 1,2,4,5-tetrahydro-3-methyl-3H-3-benzazepin-2-one 1a with various halides and sodium hydride in tetrahydrofuran-dimethylformamide solvent system was studied.Primary halides predominantly provided the 1-mono-substituted products, such as alkyl (2a-g,p,q), allyl (2j,k), propargyl (2l) and benzyl (2m-o) derivatives, in satisfactory yields, and secondary halides resulted in lower yields (2h,i) than primary halides.In attempted dialkylations with ω,ω'-dibromoalkanes, 5- and 6-membered spiro products (4c,d) were obtained by this method.The Michael type addition reaction was also studied and it was found that acrylic acid esters gave the corresponding adducts (2p,q).
