【药物名称】
化学结构式(Chemical Structure):
参考文献No.45417
标题:New cpds., their preparation and use
作者:Sauerberg, P.; Jeppesen, L.; Bury, P.S.; Murray, A.; Pettersson, I. (Novo Nordisk A/S)
来源:EP 1171414; JP 2002542218; WO 0063153
合成路线图解说明:

The Horner-Emmons condensation of 4,4'-dibromobenzophenone (I) with triethyl phosphonoacetate leads to the 3,3-diarylpropenoate (II). Ester (II) is subsequently reduced to the allylic alcohol (III) employing DIBAL in cold THF. Suzuki coupling of aryl bromide (III) with phenylboronic acid (IV) furnishes 3,3-bis-(biphenyl-4-yl)-2-propen-1-ol (V). Coupling of allylic alcohol (V) with (S) ethyl 2-ethoxy-3-(4-hydroxyphenyl)propionate (VI) by means of 1,1'-(azodicarbonyl)dipiperidine (ADDP) and tributylphosphine under Mitsunobu conditions gives rise to the ether adduct (VII). Finally, saponification of the ethyl ester group of (VII) provides the target carboxylic acid.

参考文献No.714673
标题:Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template
作者:Mogensen, J.P.; Jeppesen, L.; Bury, P.S.; Pettersson, I.; Fleckner, J.; Nehlin, J.; Frederiksen, K.S.; Albrektsen, T.; Din, N.; Mortensen, S.B.; Svensson, L.A.; Wasserman, K.; Wulff, E.M.; Ynddal, L.; Sauerberg, P.
来源:Bioorg Med Chem Lett 2003,13(2),257
合成路线图解说明:

The Horner-Emmons condensation of 4,4'-dibromobenzophenone (I) with triethyl phosphonoacetate leads to the 3,3-diarylpropenoate (II). Ester (II) is subsequently reduced to the allylic alcohol (III) employing DIBAL in cold THF. Suzuki coupling of aryl bromide (III) with phenylboronic acid (IV) furnishes 3,3-bis-(biphenyl-4-yl)-2-propen-1-ol (V). Coupling of allylic alcohol (V) with (S) ethyl 2-ethoxy-3-(4-hydroxyphenyl)propionate (VI) by means of 1,1'-(azodicarbonyl)dipiperidine (ADDP) and tributylphosphine under Mitsunobu conditions gives rise to the ether adduct (VII). Finally, saponification of the ethyl ester group of (VII) provides the target carboxylic acid.

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