200455. lajstromszámú szabadalom • Eljárás pirimidin-származékok előállítására

21

HU 200455 B

22

X

Y

Z

Q

MMR(300 MHz, ppra)

CH30

II

H

Cl

(CDCb) 8.89 (dd, J =

4.3,

1.7

Hz,

1H), 8.57 (dd, J = 8.6,

1.7

Hz,

1H),

8.38 (d, J = 5.5 Hz,

1H),

8.37

(d,

J = 7.9 Hz, 1H), 7.83 (d

. J *

= 7.9

Hz,

1H), 7.53 (dd, J = 8.8,

4.3

Hz,

1H),

6.60 (d, J = 5.5 Hz, 1H),

, 3.76 (s,

3H).

C2H50-H

H

Cl

(CDCb) 8.89 (dd, J = 4.1

, 1.4

Hz,

1H),

8.56 (dd, J = 8.8, 2.0

Hz,

1H),

8.38

(d, J = 5.7 Hz, 1H), ;

8.36

(d,

J =

= 8.0 Hz, 1H), 7.82 (d,

J =

: 7.9

Hz,

1H), 7.53 (dd, J = 8.6,

4.2

Hz,

1H),

6.56 (d, J = 5.6 Hz, 1H), 4.17

(quart., J = 7.0 Hz, 2H),

1.12

(t,

J =

= 7.1 Hz, 3H).

CH3-H

II

(CH3)2N(DMSO-d6) 8.71 (d, J =

3.0

Hz,

1H),

8.62 (d, J = 5 Hz, 1H),

8.51

(d,

J =

= 8 Hz, 1H), 8.04 (d, J

= 8

Hz,

1H),

7.50 (dd, J = 8, 3 Hz,

1H),

7.42

(d,

J = 5 Hz, 1H), 2.93

(s, 1

BH),

2.48

(s, 3H).

CH3

H

H

F

(DMSO-d6) 8.85 (d, J = 4

Hz,

1H),

8.62

(d, J = 5 Hz, 1H), 8.56

(d, J

= 9

Hz,

1H), 8.22 (dd, J = 8, 6

Hz,

1H),

7.74

(dd, J = 10, 8 Hz, 1H),

7.67

(dd,

J =

= 9, 4 Hz, 1H), 7.44 (d, J

r = 5

Hz,

1H),

2.46 (s, 3H).

CH30

H

CH3-Cl

(DMSO-d6) 8.91 (dd, J =

4.3,

, 1.7

Hz,

1H), 8.64 (dd, J = 8.8,

1.5

Hz,

1H),

8.20 (d, J = 7.9 Hz, 1H),

8.08

: (d,

J =

= 7.9 Hz, 1H), 7.75 (dd, .

J =

8.7,

4.3 Hz, 1H), 6.83 • (s,

1H),

3.52

(s,

3H), 2.35 (3

, 3H).

CH30(CH2)z

OH

11

H

(CDCb) 8.86 (dd, J = 4.1

, 1.4

Hz,

1H),

8.43 (dd, J = 7.2, 1.5

Hz,

1H),

8.41

(d, J = 5.6 Hz, 1H), 8.19

(dd,

J =

8.5,

1.4 Hz, 1H), 7.94 (bd, J =

= 7.8

Hz,

1H),

7.74 (t, J = 7.4 Hz, 1H),

7.43

(dd,

J =

= 8.6, 4.2 Hz, 1H), 6.64 (d, J

= 5.5

Hz,

1H), 4.26 (sep., J = 3.1

Hz,

2H),

3.44

(t, J = 4.3 Hz, 2H),

3.27

(s,

3H).

C2H50-CH3-H

H

(DMSO-d6) 8.86 (dd, J =

4, 2

Hz,

1H),

8.43 (dd, J = 7, 2 Hz,

1H),

8.22

(s,

1H), 8.17 (dd, J = 9, 2

Hz,

1H),

7.91

(dd, J = 8, 2 Hz, 1H),

7.73

(t,

J =

= 8 Hz, 1H), 7.41 (dd, ,

J =

9, 4

Hz,

1H), 4.15 (quart., 3 = 1

Hz,

2H),

2.02

' (s, 3H), 1.07 (t, J = 7 Hz, 3H).

C2

H50-H

CH3-Cl

(DMSO-d6) 8.91 (dd, J =

4.1,

1.4

Hz,

1H), 8.64 (dd, J = 8.8,

1.4

Hz,

1H),

8.20 (d, J = 7.9 Hz, 1H),

8.09

(d,

J =

= 7.9 Hz, 1H), 7.75 (dd, J

r =

8.8,

4.2 Hz, 1H), 6.79 (s, 1H),

3.90

(quart.,

J = 7.0 Hz, 2H), 2.37

(s, 3H),

0.85

(t, J = 6.9 Hz, 3H).

13