- Synthesis of 6-oxopyrimidin-1(6H)-yl benzamide derivatives and evaluation of their antibacterial and cytotoxic activity
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A series of novel 2-alkylamino and 2, 4-dialkyl amino 6-oxopyrimidin-1(6H)-yl) benzamide derivatives were prepared in good yields from a base-catalyzed ring opening of oxadiazolo[3,2-a]pyrimidin-5-one and evaluated for their antibacterial and cytotoxicity. Most of the compounds exhibited antibacterial activity. In particular, compounds 5b and 5k exhibited considerable antibiotic activity against Klebsiella pneumonia and Bacillus cereus. In addition, compounds 5g and 5i also inhibited the growth of two human tumor cell lines (A549 and H460) at micromolar concentrations.
- Devarasetty, Kiran,Tharikoppula, Giri,Sridhar, Tailor,Eppakayala, Laxminarayana,Kyasani, Mahesh,Arumugam, Premkumar,Pusuluri, Srinivas
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p. 263 - 274
(2016/03/09)
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- A protection strategy substantially enhances rate and enantioselectivity in ω-transaminase-catalyzed kinetic resolutions
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The kinetic resolution of 3-aminopyrrolidine (3AP) and 3-aminopiperidine (3APi) with ω-transaminases was facilitated by the application of a protecting group concept. 1-N-Cbz-protected 3-aminopyrrolidine could be resolved with >99% ee at 50% conversion, the resolution of 1-N-Boc-3-aminopiperidine yielded 96% ee at 55% conversion. The reaction rate was up to 50-fold higher by using protected substrates. Most importantly, enantioselectivity increased remarkably after carbamate protection compared to the unprotected substrates (86 vs. 99% ee). Surprisingly, benzyl protection of 3AP had no influence on enantioselectivity. A possible explanation for this observation could be the different flexibility of the benzyl- or carbamate-protected 3AP as confirmed by NMR spectroscopy.
- Hoehne, Matthias,Robins, Karen,Bornscheuer, Uwe T.
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body text
p. 807 - 812
(2009/04/10)
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- PROCESS FOR PRODUCING NITROGENOUS HETEROCYCLIC COMPOUND
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A nitrogenous heterocyclic compound such as 3-aminopyrrolidine derivative is produced by hydrogenolysis of an N-substituted nitrogenous heterocyclic compound with normal pressure hydrogen in a water-based solvent in presence of a catalyst. In the case an optically active 1-substituted-3-aminopyrrrolidine derivative is used as a raw material, an optically active 3-aminopyrrolidine derivative can be obtained as a product practically without racemination.
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Page/Page column 10
(2010/11/08)
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- Methods for making optically active 3-aminopyrrolidine-2,5-dione derivative and optically active 3-aminopyrrolidine derivative
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A method for making an optically active 3-aminopyrrolidine-2,5-dione derivative represented by the formula (3) includes cyclizing an optically active asparagine ester derivative represented by the formula (1) or (2), or an acid salt thereof. A method for making an optically active 3-aminopyrrolidine derivative represented by the formula (9) includes reducing the optically active 3-aminopyrrolidine-2,5-dione derivative represented by the formula (3). A method for making an optically active 3-aminopyrrolidine derivative includes hydrogenolyzing the optically active 3-aminopyrrolidine derivative represented by the formula (9).
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Page column 14
(2008/06/13)
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- Methods for making optically active 3-aminopyrrolidine-2,5-dione derivative and optically active 3-aminopyrrolidine derivative
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A method for making an optically active 3-aminopyrrolidine-2,5-dione derivative represented by the formula (3) includes cyclizing an optically active asparagine ester derivative represented by the formula (1) or (2) or an acid salt thereof. The optically active 3-aminopyrrolidine-2,5-dione derivative represented by the formula (3) may be reduced to form an optically active 3-aminopyrrolidine derivative represented by the formula (9). When, in the formula (9), R1 is an unsubstituted or substituted benzyl group, the compound may be hydrogenated to obtain the corresponding 1-unsubstituted compound in which R1 is hydrogen.
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- Novel platinum complex, antineoplastic agent containing the same, and intermediate therefor
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Novel platinum complex of the formula: STR1 wherein n is an integer of 1 or 2 and A is a ligand of the formula: STR2 which has excellent antineoplastic activity and is useful as an antineoplastic agent for the treatment of various malignant tumors, and a pharmaceutical composition containing the platinum complex as an active ingredient, and an intermediate for preparing the compound.
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