• 제목/요약/키워드: Convergent synthesis

검색결과 44건 처리시간 0.02초

An Improved Convergent Approach for Synthesis of Erlotinib, a Tyrosine Kinase Inhibitor, via a Ring Closure Reaction of Phenyl Benzamidine Intermediate

  • Asgari, Davoud;Aghanejad, Ayuob;Mojarrad, Javid Shahbazi
    • Bulletin of the Korean Chemical Society
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    • 제32권3호
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    • pp.909-914
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    • 2011
  • An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized.

Convergent Synthesis of PAMAM-like Dendrimers from Azide-functionalized PAMAM Dendrons

  • Lee, Jae-Wook;Kim, Jung-Hwan;Kim, Byung-Ku;Kim, Ji-Hyeon;Shin, Won-Suk;Jin, Sung-Ho;Kim, Myung-hak
    • Bulletin of the Korean Chemical Society
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    • 제27권11호
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    • pp.1795-1800
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    • 2006
  • The convergent synthesis of symmetric PAMAM-like dendrimers from azide-functionalized poly(amido- amine) (PAMAM) dendrons and two different multi-alkynes was investigated. The stitching method was based on the click chemistry protocol, i.e., the copper-catalyzed cycloaddition reaction between an alkyne and an azide.

코팅 피치의 물성제어를 통한 흑연 음극재의 전기화학 성능 향상 연구 (A Study on the Improvement of the Electrochemical Performance of Graphite Anode by Controlling Properties of the Coating Pitch)

  • 김보라;김지홍;강석창;임지선
    • 공업화학
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    • 제33권5호
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    • pp.459-465
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    • 2022
  • 천연 흑연의 전기화학적 특성 향상을 목적으로 피치 코팅을 실시하였다. 최적 코팅용 피치의 합성조건을 알아보기 위해 다양한 온도에서 합성된 피치를 코팅하여 음극 특성을 알아보았다. 합성온도가 증가할수록 연화점, 잔탄율이 증가하며 열적 안정성이 높아졌으나, 430 ℃에서는 과한 축합반응으로 NI (NMP Insoluble)가 다량 합성되었다. 높은 열적 안정성으로 표면의 균일도와 코팅 두께가 증가함에 따라 제조된 음극재의 향상된 초기쿨롱효율과 출력특성의 결과를 얻을 수 있었다. 하지만 과한 NI가 함유된 피치로 코팅한 음극재는 코팅이 실시되지 않은 흑연보다 저하된 전기화학 특성을 나타냈다. NI는 분산성이 낮고 열처리 후 구체 형성의 영향으로 불균일한 SEI층 형성에 기인한다는 결과를 얻을 수 있었다. 피치 합성온도를 제어하여 균일한 표면과 적절한 코팅층 형성이 이루어지는 최적 조건을 도출하였다.

Concise Synthetic Approaches to Naturally Occurring β-Hydroxypyranochalcones: First Total Synthesis of Purpurenone, Its Derivative, and Praecansone B

  • Wang, Xue;Lee, Yong-Rok;Kim, Sung-Hong
    • Bulletin of the Korean Chemical Society
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    • 제33권8호
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    • pp.2647-2650
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    • 2012
  • The total synthesis of biologically interesting ${\beta}$-hydroxypyranochalcones, purpurenone (1), its derivative 2, praecansone B (3), and pongapinone A (4) has been accomplished starting from commercially available 2,4-dihydroxyacetophenone or 6-methoxy-2,4-dihydroxyacetophenone in 3 steps by a convergent strategy through benzopyran formations, O-methylations, and coupling reactions.

A Convergent Synthetic Study of Biologically Active Benzofuran Derivatives

  • Hu, Kun;Jeong, Jin-Hyun
    • Archives of Pharmacal Research
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    • 제29권6호
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    • pp.476-478
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    • 2006
  • In order to construct a benzofuran library, we developed a model study of benzbromarone. Synthesis has been achieved in 53% overall yield, starting from phenol via the key intermediate 2-ethylbenzofuran which was afforded by intramolecular Wittig reaction.