- Silver-Catalyzed Isocyanide Insertion into N?H Bond of Ammonia: [5+1] Annulation to Quinazoline Derivatives
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A silver-catalyzed [5+1] annulation of o-acylaryl isocyanides with ammonium acetate and hydroxlamine was developed for the efficient and practical synthesis of quinazolines and quinazoline 3-oxides in good to excellent yields, respectively. The domino process involved an unprecedented isocyanide insertion into the N?H bond of ammonia or hydroxylamine and followed by condensation reaction at ambient conditions. (Figure presented.).
- Zhang, Lingjuan,Li, Juanjuan,Hu, Zhongyan,Dong, Jinhuan,Zhang, Xian-Ming,Xu, Xianxiu
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supporting information
p. 1938 - 1942
(2018/04/02)
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- ALKYL, FLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS
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Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein: R1 is CH2CH2CF3; R2 is CH2(cyclopropyl), CH(CH3)(cyclopropyl), or CH2CH2CH3/
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Paragraph 00278
(2014/04/04)
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- FLUOROALKYL AND FLUOROCYCLOALKYL 1,4-BENZODIAZEPINONE COMPOUNDS AS NOTCH|INHIBITORS
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Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is -CH2CH2CF3; R2 is -CH2CH2CH2F, -CH2CF2CH3, -CH2CH
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Paragraph 00201; 00205
(2014/04/04)
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- BENZODIAZEPINE CGRP RECEPTOR ANTAGONISTS
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The present invention is directed to compounds of Formula I: I (where variables R1, R2, R3, R6, R7, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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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- Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: A novel series of 5-HT2A/2C receptor antagonists. Part 2
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Following the programme started at Janssen Research Foundation searching for 5-HT2A/2C antagonists, we now report on the synthesis of a series of substituted 2-(Dimethylaminomethyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a] azepine derivatives. The 5-HT2A, 5-HT2C and H1 receptor affinities as well as the mCPP antagonistic activity of the compounds synthesised is described.
- Ignacio Andres,Alcazar, Jesus,Alonso, Jose M.,Diaz, Adolfo,Fernandez, Javier,Gil, Pilar,Iturrino, Laura,Matesanz, Encarna,Meert, Theo F.,Megens, Anton,Sipido, Victor K.
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p. 249 - 253
(2007/10/03)
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- 3-Benzoyl-2-nitrophenylacetic acids, metal salts, amides and esters
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3-Benzoyl-2-nitrophenylacetic acids, metal salts, amides and esters are disclosed having the formula: STR1 wherein R1 is hydrogen or lower alkyl; R2 is OH, OM, O-lower alkyl, NH2, NH-lower alkyl or N,N-dilower alkyl; X is
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