201768. lajstromszámú szabadalom • Eljárás új cef-3-em-4-karbonsav-származékok és ilyen vegyületeket tartalmazó gyógyászati készítmények előllítására

HU 201768 B

17

18

A példa száma

Vegyidet

g-A>3

R2ésR3

Fiziko-kémiai jellemzők

24.

R2 = -3-NHj R =

= 5-CH2OH

00.: 170-175 °C (bomlik)

IRv max (cm'1): 1770,1690 NMR (D20 + CF3C02D) 8:2,20-2,75 (2H, m), 3,35-3,68 (2H, m), 3,30 (1H, d, J = 18Hz), 3,75 (1H, d, J = 18Hz), 4,78 (2H, s), 5,15 (1H, t, J = 8Hz), 5,23 (1H, d, J = 15Hz), 5,36 (1H, d, J =5Hz), 5,68 (1H, d, J = 15Hz), 5,92 (1H, d, J = 5Hz), 7,21 (1H, s), 7,65-7,75 (1H, m), 8,10-8,20 (2H, m)

25.

r2=

= 3-NH2 r3=

= 5-CONH2

op.: 176-181 °C (bomlik)

IRv max (cm'1): 1775,1690,1595-1640 NMR (D20 + CF3C02D) 8:2,10-2,75 (2H, m),

3,35-3,60 (2H, m), 3,20-3,39 (2H, m) 5,16 (1H, t, J = 9Hz), 5,25-5,81 (2H, m), 5,35 (lH,d,J=5Hz), 5,91 (1H, d, J=5Hz), 7,20 (1H, s), 8,01-8,11 (1H, m), 8,38-8,49 (1H, m).

26.

r2=

3-NH2

r3=

= 5-Cl

op.: 160-170 °C (bomlik)

IRv max (cm'1): 1770,1690,1610 NMR (D20 + CD3CN) 8: 2,10-2,60 (2H, m), 3,20-3,50 (2H, m), 3,08-3,75 (2H, m), 4,90 (1H, t, J = 9Hz), 4,80-5,50 (2H, m), 5,13 (1H, d, J=5Hz), 5,72 (1H, d, J = 5Hz), 6,86 (1H, s), 7,52-7,61 (1H, m),

8,18-8,28 (2H, m)

27. R2 =

= 3-CH2OH

r3=

= 5-OCH3

(sz=széles)

op.: 180-190 °C (bomlik)

NMR (D20) 8:2,1-2,7 (2H, m), 3,17 (1H, d, J = 18Hz),

3,1-3,7 (2H, m), 3,65 (1H, d, J = 18Hz), 3,97 (3H, s), 4,78 (2H, s), 4,98 (1H, t, J=7Hz), 5,22 (1H, d, J = 5Hz), 5,23 (1H, d, J = 14Hz), 5,52 (1H, d, J = 14Hz), 5,77 (1H, d, J = 5Hz), 6,83 (1H, s), 7,91 (1H, sz s), 8,45 (1H, sz s), 8,55 (1H, szs)

28.

r2=

=3-CONH2

r3=

= 5-OCH3

op.: 165-180 °C (bomlik)

NMR (D20 + CF3COOD) 8:2,1-2,7 (2H, m), 3,15-3,90 (4H, m), 4,10 (3H, s), 5,10 (1H, t, J = 8Hz), 5,29 (1H, d, J=5Hz), 5,35 (1H, d, J = 15Hz), 5,75 (1H, d, J = 15Hz), 5,84 (1H, d, J = 5Hz), 7,10 (1H, s), 8,35-9,0 (3H, m)

29.

r2=

l3'F

r3=h

op.: 175-190 °C (bomlik)

NMR (D20) 8:2,0-2,6 (2H, m), 3,2-3,8 (4H, m),

4,93 (1H, t, J=7Hz), 5,17 (1H, d, J = 5Hz), 5,28 (1H, d, J = 15Hz), 5,57 (1H, d, J=15Hz), 5,73 (1H, d,J=5Hz), 6,89 (1H, s), 7,8-9,0 (4H, m)

30. R2=3-= -NHCOCH2OH R = H

(sz = széles)

op.: 180-200 °C (bomlik)

NMR (D20) 8:2,1-2,7 (2H, m), 3,15 (1H, d, J = 18Hz),

3,1-3,6 (2H, m), 3,63 (1H, d, J = 18Hz), 4,22 (2H, s), 4,83 (lH,t,

J = 7Ht), 5,18 (1H, d, J = 5Hz), 5,32 (1H, d, J = 7Hz), 5,54 (1H, d, J = 7Hz), 5,74 (1H, d, J = 5Hz), 6,79 (1H, s), 7,86 (1H, d, d, J = 8Hz, J = 6Hz), 8,38 (1H, d, J=8Hz), 8,57 (1H, d, J=6Hz), 9,33 (1H, sz s)

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