- Formation of Enamines via Catalytic Dehydrogenation by Pincer-Iridium Complexes
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Di-isopropylphosphino-substituted pincer-ligated iridium catalysts are found to be significantly more effective for the dehydrogenation of simple tertiary amines to give enamines than the previously reported di-t-butylphosphino-substituted species. It is
- Lu, Yansong J.,Zhang, Xiawei,Malakar, Santanu,Krogh-Jespersen, Karsten,Hasanayn, Faraj,Goldman, Alan S.
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supporting information
p. 3020 - 3028
(2020/03/23)
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- SUBSTITUTED NITROGEN CONTAINING COMPOUNDS
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Disclosed are compounds of Formula (I): or a salt thereof, Formula (II) wherein R1 is: or; each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
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Page/Page column 274
(2019/01/05)
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- SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 39; 40
(2014/10/29)
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- BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Paragraph 0561
(2013/08/28)
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- 2-(arylimino-methyl)-3-dialkylaminoacrylonitriles, a process for their preparation and their use
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2-(Arylimino-methyl)-3-dialkylaminoacrylonitriles can be obtained by reaction of β-anilino-acrylonitriles with ortho-formamides. They are suitable as starting substances for the preparation of 4-amino-5-iminiummethylene-2-pyrimidines or 4-amino-5-formyl-2
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- Process for the preparation of 2,5-disubstituted pyridines
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2,5-Disubstituted pyridines of the formula STR1 can be prepared by reacting enamines of the formula STR2 with β-amino-acrylonitriles of the formula STR3 and treating the open-chain intermediate, which represents a R-R1 -5-amino-penta-2,4-dienonitrile, with protic acids or with ammonia.
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- A One Pot Synthesis of β-Cyanoenamines
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Orthoesters, cyanoacetic acid and secondary amines react together, in a one step procedure, to produce β-cyanoenamines.
- Rene, Loic,Poncet, Joeel,Auzou, Gilles
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p. 419 - 420
(2007/10/02)
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- Method of preparing β-alkoxyacrlonitriles
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A process for the preparation of a β-alkoxyacrylonitrile of the formula where R is hydrogen or an alkyl moiety, among others, by contacting a compound of the formula where Me is an alkali metal or alkaline earth metal and α is 1 or 2 respectively, an elevated temperature with a halogen compound of the formula where R' is among others a straight or branched alkyl or alkenyl moiety and Hal represents chlorine, bromine, or iodine. Also disclosed is a process for preparing a 3-amino-acrylonitrile of the formula STR1 where R5 and R6 represent, among others, hydrogen, alkyl or alkenyl by contacting a 3-alkoxyacrylonitrile or a metal salt of 3-hydroxyacrylonitrile with ammonia and/or amine. Also disclosed is a process for the preparation of such 3-aminoacrylonitrile by contacting a 3-alkoxyacrylonitrile of the formula STR2 where R' has the meaning given above and R7 has the same meaning as R stated above with an amine of the formula STR3 wherein R5 and R6 represent among others hydrogen, alkyl or alkenyl. The application further discloses a process for preparing a 3-amino-acrylonitrile of the formula STR4 where R5, R6 and R7 have the above meanings by contacting a compound of the formula EQU1 with an amine. The Application also discloses the preparation of two-cyanovinyl esters by reaction of a cyanovinyl compound of the formula EQU2 with an acid halide or an acid anhydride.
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- AMINOPHOSPHONIC ACID AND AMINOPHOSPHINIC ACID ANALOGUES OF ASPARTIC ACID
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4-Oxoazetidin-2-ylphosphonates and phosphinates, obtained from Arbusov reactions of 4-acetoxyazetidin-2-one and 4α-acetoxy-3β-phthalimido-2-one with a variety of phosphites and phosphonites, were hydrolysed to β-phosphono- and β-phosphino β-alanine (phosphono- and phosphinoaspartic acid) derivatives.In model studies for their incorporation in peptides, conditions for the selective removal of protecting groups for carboxylic acids, phosphonic and phosphinic acids, and amines, in derived di- and tripeptides were investigated.Alanyl and alanyl alanyl peptide incorporation into bacteria was studied.
- Campbell, Malcolm M.,Carruthers, Nicholas I.,Mickel, Stuart J.
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p. 2513 - 2524
(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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- Process for producing dialkyl aminoacrylonitrile
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A process for producing a dialkyl aminoacrylonitrile by treating dimethylaminopropionitrile with a hydrogen acceptor in the presence of a dehydrogenation catalyst. The dialkylaminoacrylonitrile thus produced is converted to aminomethylene malonitrile, a known intermediate for thiamine.
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