Trimethoprim 중간체인 Diethyl 3,4,5-Trimethoxybenzylmalonate의 새로운 합성

A New Route to Diethyl 3,4,5-Trimethoxybenzylmalonate, a Trimethoprim Intermediate

  • 정봉영 (고려대학교 이과대학 화학과) ;
  • 이채호 (고려대학교 이과대학 화학과)
  • 발행 : 1985.10.20

초록

3,4,5-trimethoxybenzoyl chloride와 diethyl malonate를 축합시킨 후, 염소화반응 및 가수소화 분해 반응을 거쳐 diethyl 3,4,5-trimethoxybenzylmalonate를 70%의 수득율로 합성하였다.

Direct condensation of 3,4,5-trimethoxybenzoyl chloride with diethyl malonate followed by chlorination and hydrogenolysis afforded diethyl 3,4,5-trimethoxybenzylmalonate in 70% overall yield.

키워드

참고문헌

  1. J. Amer. Chem. Soc. v.73 E.A. Falco;S. DuBreuil;G.H. Hitchings
  2. U.S. Pat. 2,909,522;Chem. Abstr. v.56 G.H. Hitchings;B. Roth
  3. J. Med. Pharm. Chem. v.5 B. Roth;E. A. Falco;G. H. Hitchings;S.R.M. Bushby
  4. J. Med. Chem. v.24 B. Roth;E. Aig;B.S. Rauckman;J.Z. Ferone;S.R.M. Bushby;C.W. Sigel
  5. Org. Syn. Coll. v.3 E.B. Hershberg;J. Cason
  6. J. Chem. Soc. D.C. Ayres;B.G. Carpenter;R.C. Denny
  7. J. Org. Chem. v.28 P. Stenbuck;R. Baltzly;H.M. Hood
  8. German Pat. 2,010,166;Chem. Abstr. v.74 R.M. Cresswell;J.W. Mentha;R. Seaman
  9. Fin. Chem. Lett. J. Paasivirta;T. Asunta
  10. J. Med. Chem. v.23 B. Roth;J.Z. Strelitz;B.S. Rauckman
  11. Japan Pat. 74 04462;Chem. Abstr. v.81 T. Tokutake
  12. British Pat. 1,468,374;Chem. Abstr. v.87 N. Tokutake
  13. German Pat. 2,443,080;Chem. Abstr. v.83 B. Alhede;N. Gelting
  14. German Pat. 2,443,079;Chem. Abstr. v.83 B. Alhede;N. Gelting
  15. J. Amer. Chem. Soc. v.71 W. Reeve;J.D. Sterling, Jr.
  16. Synthesis K. Friedrich;H.K. Thieme