200455. lajstromszámú szabadalom • Eljárás pirimidin-származékok előállítására

11

HU 200455 B

12

X Y Z Q

CH3OH II H

JÓOH H H

C2H5OH H H

(CHahNH H H

/CH2OH H H

CH3OH CH3OH

jdNHH H H

NH2- H H H

MMR{300 MHz, ppm)

(CDCh) í

8.87

(dd,

J =

4.3,

2,3

Hz,

1H),

8.45

(dd, J =

= 7.2,

1.5

Hz,

1H),

8.4

(dd,

J

= 5.6,

1.1

Hz,

1H),

8.19

(dd,

J=

8.8

, 2.1

Hz,

1H),

7.95

(d,

J =

8.3

Hz,

1H), 7.75 (t

. J

= 7.2

Hz,

1H),

7.43

(dd, J :

= 8.4,

4.1

Hz,

1H)

6.59

(dd,

, J

O

CD

II

1.1

Hz,

1H),

3.73

(s, 3H).

(CDCh) 8.7 (dd, J

= 4.3

, 1.7

Hz,

1H),

8.59

(d, .

J =

6.1 Hz,

, 1H),

8.31

(dd,

J =

= 7.2,1.3

Hz,

1H),

8.15

(dd,

J =

8.1,

1.6 Hz, 1H), 7.9 (dd, J = 8.3, 1.3 Hz, 1H), 7.66 (dd, J = 9.0, 7.7 Hz, 1H), 7.38 (dd, J = 8.1, 4.3 Hz, 1H), 7.13 (m, 3H), 6.74 (d, J = 5.5 Hz, 1H), 6.7 (m, 2H).

(CDCh)

8.85

(dd,

J =

4.3, 1.7

Hz,

1H)

8.42

(d,

J

= 5.3 Hz, 1H)

8.38

(d,

J =

5.5

Hz,

1H),

8.17 (dd,

J =

8.8,

1.7

Hz,

1H),

7.92

(bd,

J = 8.3

Hz,

1H),

7.72

(t,

J ■

= 7.2

: Hz,

, 1H), 7.42

(dd,

J =

8.S

1 4.4

Hz,

1H)

1, 6.54

(d,

J =

= 5.5 Hz,

1H),

4.13

(dq, J =

6.8,

1.5

Hz,

2H),

1.07

(t,

J = 6.8

Hz,

3H).

(CDCh)

8.88

(dd,

J =

4.1, 1.4

Hz,

1H)

8.4

(dd,

J

= 7.

3, 1.6 Hz,

1H),

8.14

(dd,

J =

= 8.2

, 1.7

Hz,

1H), 8.1

(d,

J =

= 6.4 Hz,

1H),

7.87

(dd, J =

8.2,

1.4

Hz,

1H),

7.68

(t,

J = 7.8

Hz,

1H),

7.39

(dd, J

= 8.2, 4.3 Hz,

1H),

6.19

(d,

J =

: . 6.4

Hz,

1H)

1 2.84 1

(bs,

6H).

(CDCh)

8.86

(dd,

J =

4.3, 1.9

Hz,

1H),

8.46

(m,

2H),

8.2

(dd,

J = 8.5

, 1.8

Hz,

1H),

7.95 (dd, J

= 8.3, 1.3

Hz,

1H),

7.75

(t,

J i

= 7.8

1 Hz,

, 1H), 7.43

(dd,

J =

8.1,

4.3

Hz,

1H),

7.23-7.26 (re

3H)

7.14--7.17

(m,

2H),

6.63 (d, J

=5.5

Hz,

1H),

5.16

(AB,

J =

12.2

Hz, 2H).

(CDCh)

8.97

(dd,

J =

4.3, 1.6

Hz,

1H),

8.28

(dd

. J -: 7.2,

1.3

Hz, 1H),

8.2

(dd,

J =

8.1,

1.6

Hz, 1H)

, 7.94 (dd,

, J =

7.7,

1.3

Hz,

1H),

7.7 (t

, J

= 7.8

Hz,

1H),

7.48

(dd

, J

= 8.3,

4.1

Hz,

1H),

7.07

(s,

1H),

3.92 (s,

3H),

3.66

(s.

3H).

(CDCh) 8.91

(dd, J

= 4

.3, 1.6

i Hz,

1H),

8.43

(dd

> J

= 7.2,

1.4

Hz,

1H),

8.18

(dd,

J

= 8.4, 1.9

Hz,

1H),

8.12

(d,

J =

5.8

Hz,

1H), '

7.94

(dd,

J =

8.3,

1.4

Hz,

1H),

7.73 (t, J

= 7.8

Hz,

1H),

7.57

(bs

;, 1H), 7.42 I

Idd,

J =

8.2

4.3

Hz,

1H),

7.06-7.24

(in,

5H),

6.55

(d, J = 6.0 Hz, 1H).

(DMSO-de) 8.81 (dd, J = 4.3, 1.6 Hz, Ili), 8.47 (dd, J = 8.1, 1.3 Hz, 1H), 8.17 (d, J = 8.4 Hz, 1H), 8.17 (d, J = 7.4 Hz, 1H), 7.96 (d, J = 6.0 Hz, 1H), 7.86 (dd, J =

8