?????????Alimta?????

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?????????Alimta?????
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contents
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1953? ????(Methotrexate) ??
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1985?Edward C. Taylor????DDATHF1
1???????????? 2????????-N-H 3?6??????
1992?Edward C. Taylor????Alimta2
1 J.Med.Chem., 1985, 28, 914 2 J.Med.Chem.,
1992, 35, 4450
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??Eli Lilly??2004?????? ????????,???Alimta,
??LY231514? ?????????????? ?????????????? ??????
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??????? Dihydrofolate reductase ??????
Thymidylate synthase ???????????? Glycinamide
ribonucleotide formyltransferase ??????????????
Aminoimidazole ribonucleotide formyltransferase ?
?????? Tetrahydrofolate synthase enzyme
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Yield 21.2 Ref Edward C.Taylor, J.Med.Chem.,
1992, 35, 4450
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BSA N,O-?(??????)??? Ref Charles J. Barnett, US
5426187 (1995)
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Yield 31.1
US 5416211 (1995), Org. Proc. Res. Dev., 1999, 3,
184 ????????, 2006, 37, 798 EP 905128 (1999)
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Ref Edward C. Taylor, US 5254687 (1993)
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Yield 14.9 Ref Edward C. Taylor, Tetrahedron
Lett., 1999, 40, 4023 Edward C. Taylor,
US 6066732 (2000) Edward C. Taylor, J.
Org. Chem., 2003, 68, 9938
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Yield 2.9 Ref ???, ????????, 2005, 36, 727
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Yield7.66
Tetrahedron Lett., 40, 5291 J. Org. Chem., 66,
3726
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Ref Charles J. Barnett, US 5416211 (1995)
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Yield 21.7 Ref Tetsuo Miwa, J. Org. Chem.,
1993, 58, 1696
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Yield 4.8 Ref ???,????, 2006, 26, 546
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Yield 25.8 Ref CN 101085775
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Thank you for your kind attentions!
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