Piperidin-4-ol → 6-n-Propyl-3-(4-hydroxy-1-piperidinyl)pyridazine
反応式
[CH3:1][C:2]1[N:7]=[N:6][C:5](Br)=[CH:4][CH:3]=1.[CH3:9][CH2:10]N(C(C)C)C(C)C.[OH:18][CH:19]1[CH2:24][CH2:23][NH:22][CH2:21][CH2:20]1>>[CH2:1]([C:2]1[N:7]=[N:6][C:5]([N:22]2[CH2:23][CH2:24][CH:19]([OH:18])[CH2:20][CH2:21]2)=[CH:4][CH:3]=1)[CH2:9][CH3:10]参加物
4
実験手順
Following a procedure similar to that of Example 3, 81 millimoles of 6-methyl-3-bromopyridazine was combined with 16 mL DIPEA and 163 mmoles of 4-hydroxypiperidine and heated to 120° for 16 hours to obtain 6-methyl-3-(4-hydroxy-1-piperdinyl)pyridazine (Formula IV: Y=bond, R=CH3) in 24% yield. 6.8 Mmols of the latter and 7.4 mmoles of 2-methyl-5-(4-hydroxy-3,5-dimethyl phenyl)-2H-tetrazole (Formula III: R2 =R3 =R4 =CH3) were reacted with equimolar amounts of DEAD and TPP essentially as described above in Example 1c. Recrystallization from methanol gave a 74% yield of the compound of Formula I (R1 =R2 =R3 =R4 =CH3, Y=bond), m.p. 188°-189° C.