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Volumn 16, Issue 20, 2014, Pages 5422-5425

Asymmetric synthesis of highly functionalized tetrahydropyran DPP-4 inhibitor

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE IV INHIBITOR; ENZYME INHIBITOR; GLYCINE; PYRONE DERIVATIVE; RUTHENIUM;

EID: 84908060768     PISSN: 15237060     EISSN: 15237052     Source Type: Journal    
DOI: 10.1021/ol502661g     Document Type: Article
Times cited : (33)

References (32)
  • 2
    • 84908080993 scopus 로고    scopus 로고
    • note
    • Since sitagliptin, the first DPP-4 inhibitor was approved by the FDA in 2006, several additional DPP-4 inhibitors, including valdagliptin, saxagliptin, linagliptin, and alogliptin are on the market.
  • 20
    • 84908080991 scopus 로고    scopus 로고
    • note
    • For example, the procedure reported in ref 8a was cumbersome to run and the yields obtained in our lab were not as high as quoted.
  • 21
    • 84908080990 scopus 로고    scopus 로고
    • note
    • It is not recommended to use propargyl bromide on large scale due to safety concerns.
  • 22
    • 84908080989 scopus 로고    scopus 로고
    • note
    • The addition mode has been studied in-depth, but its mechanism to suppress the formation of byproducts remains unclear.
  • 23
    • 84908080988 scopus 로고    scopus 로고
    • note
    • Alternatively, the inorganic salts could be removed by filtration.
  • 28
    • 84908080987 scopus 로고    scopus 로고
    • note
    • Preliminary results showed that Au-catalyzed cyclization led to an undesired 5-exo dig cyclization/isomerization.
  • 29
    • 84908080986 scopus 로고    scopus 로고
    • note
    • 2, no desired product was observed.
  • 31
    • 84908080985 scopus 로고    scopus 로고
    • note
    • 9
  • 32
    • 84908080984 scopus 로고    scopus 로고
    • note
    • Overoxidation of 6 was suppressed at 0 ° C.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.