- One-pot preparation of carbamoyl benzotriazoles and their applications in the preparation of ureas, hydrazinecarboxamides and carbamic esters
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Carbamoyl benzotriazoles were conveniently synthesized in one-pot from carboxylic acids, diphenyl phosphorazidate (DPPA) and 1H-benzotriazole (BtH). The reactivity and applications of carbamoyl benzotriazoles were also explored. Carbamoyl benzotriazoles react smoothly with amino acids, hydrazines and alcohols, thus providing facile access to the corresponding ureas, hydrazinecarboxamides and carbamic esters, respectively, in good to excellent yields.
- Mao, Hui,Liu, Huili,Tu, Yawei,Zhong, Zhiyun,Lv, Xin,Wang, Xiaoxia
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- Carboxamide derivatives and their use in the treatment of thromboembolic diseases and tumours
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Compounds of the formula (I), in which the variables have the following meaning, D is phenyl or pyridyl, each of which is unsubstituted or monosubstituted or polysubstituted by Hal, A, OR2, N(R2)2, NO2, CN, COOR
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- Novel glycine transporter type-2 reuptake inhibitors. Part 1: α-amino acid derivatives
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A variety of α-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [ 14C]-glycine in COS7 cells transfected with human glycine transporter-2 (hGlyT-2) was evaluated. An array of substituents at the chiral center was studied and overall, L-phenylalanine was identified as the preferred amino acid residue. Compounds prepared from L-amino acids were more potent GlyT-2 inhibitors than analogs derived from the corresponding D-amino acids. Introducing an achiral amino acid such as glycine, or incorporating geminal substitution in the α-position, led to a significant reduction in GlyT-2 inhibitory properties.
- Wolin, Ronald L.,Venkatesan, Hariharan,Tang, Liu,Santillán Jr., Alejandro,Barclay, Tristin,Wilson, Sandy,Lee, Doo Hyun,Lovenberg, Timothy W.
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p. 4477 - 4492
(2007/10/03)
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- Supported 3,5-disubstituted chiral hydantoin: A practical catalyst for the asymmetric hydrocyanation of 3-phenoxybenzaldehyde
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A novel synthesis of six (R)-3,5-disubstituted chiral hydantoins in mixed solvent is reported. The catalysts were supported on a new polymeric resin afterwards and their enantioselectivities are examined via the asymmetric hydrocyanation of 3-phenoxybenzaldehyde.
- Zhai, Zhicai,Chen, Jinlong,Wang, Hailing,Zhang, Quanxing
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p. 1873 - 1883
(2007/10/03)
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