- NEW PROCESSES
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The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
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Page/Page column 144
(2009/08/16)
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- A NEW SYNTHESIS METHOD FOR THE PREPARATION OF N,N-DIMETHYLFORMAMIDE DI-TERT-BUTYL ACETAL
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A new synthetic method for the preparation of N,N-dimethylformamide di-tert-butyl acetal by acid catalyzed transacetalization of readily available N,N-dimethylformamide dimethyl acetal is described.
- Mohacsi, Erno
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p. 723 - 726
(2007/10/02)
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- Group Transfer Reactions. - Tetracarbonylferrates from Orthoformic Acid Derivatives and Pentacarbonyliron
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The nucleophilic leaving group X is transferred from orthoformic acid derivatives HC(NR2)X (X= NR2, OR, CN) to Fe(CO)5.No such reactions were observed between 4 and amide acetals (HCX2NR2) or ortho ester derivatives HCX3 (X= OR, SR).The structures of the transition metal-acyl complexes obtained have been determined by IR and NMR spectra.In the case of the reaction of tris(dimethylamino)methane (3a) with 4 the equilibrium between the resulting amidinium-carbamoyltetracarbonylferrate complex 5a and the starting materials was investigated.The equilibrium is shifted completely in favor of the ionic compound 5a.However, 3a could be isolated by extraction of this solution with an apolar solvent.Alkylation of 5a with triethyloxonium tetrafluoroborate leads to the tetracarbonyliron-carbene complex 13.Reaction of 5a with acrylonitrile or methyl acrylate by addition of both the nucleophile "NR2-" and the electrophile + and subsequent eliminations gives the β-dimethylamino substitution product 18 and 21, respectively.In contrast 3a induces polymerisation of acrylonitrile.
- Daub, Joerg,Hasenhuendl, Adelheid,Krenkler, Karl P.,Schmetzer, Johannes
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p. 997 - 1015
(2007/10/02)
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