반응 #2358500

ord-b95f062e2cf34926ab6257d876e644d7

반응 방정식

O=C(Cl)OCc1ccccc1
benzyl chloroformate
NC1(C(=O)O)CCCC1
1-aminocyclopentanecarboxylic acid
O=C([O-])[O-].[Na+].[Na+]
sodium carbonate
O=C(NC1(C(=O)O)CCCC1)OCc1ccccc1
carbamate
수율 87.4%
O=C(NC1(C(=O)O)CCCC1)OCc1ccccc1
N-Benzyloxycarbonyl-1-aminocyclopentane-1-carboxylic acid
수율 87.4%

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    세척the reaction mixture washed with ether
  2. 2
    추출extracted with ethyl acetate
  3. 3
    건조dried (Na2SO4)
  4. 4
    여과filtered
  5. 5
    기타the solvent removed

실험 절차

A solution of benzyl chloroformate (0.290 g, 1.1 mmol) in dioxane (2.5 cm3) was added dropwise to a solution of 1-aminocyclopentanecarboxylic acid (Fluka) (0.2 g, 1.54 mmol) and sodium carbonate (0.490 g, 4.64 mmol) in water (5 cm3) at 0° C. Stirring was continued at room temperature overnight and the reaction mixture washed with ether. The aqueous layer was acidified with 2M hydrochloric acid, extracted with ethyl acetate, dried (Na2SO4), filtered and the solvent removed to afford carbamate 21 (0.253 g, 62%) as an oil which solidified on standing. Carbamate 21 was shown to be a 70:30 mixture of conformers by 1H NMR analysis (the ratio was estimated from the integration of the resonances at δ 5.31 and 7.29-7.40, assigned to the N—H protons of the major and minor conformers, respectively): mp 70-80° C. (lit.1 82-86° C., ethyl acetate, petroleum ether); δH (400 MHz; CDCl3; Me4Si) 1.83 (4H, br s, 2× cyclopentyl-H2), 2.04 (2H, br s, cyclopentyl-H2), 2.20-2.40 (2H, m, cyclopentyl-H2), 5.13 (2H, br s, OCH2Ph), 5.31 (0.7H, br s, N—H) and 7.29-7.40 (5.3H, m, Ph and N—H*); δC (100 MHz; CDCl3) 24.6 (CH2, cyclopentyl-C), 37.5 (CH2, cyclopentyl-C), 66.0 (quat., cyclopentyl-C), 66.8 (CH2, OCH2Ph), 128.0 (CH, Ph), 128.1 (CH, Ph), 128.4 (CH, Ph), 136.1 (quat, Ph), 155.8 (quat., NCO2) and 179.5 (quat., CO2H). * denotes resonance assigned to minor conformer.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US09119851B2uspto-grants-2015_09