186583. lajstromszámú szabadalom • Eljárás új 2-(kívánt esetben szubsztituált)-amino-karbonil-oxi-alkil-1,4-dihidropiridin származékok előállítására

1

2

186 583

7. táblázat i

Pld

sz.

ÍR (KBr): cm

1

1H NMR (90 MHz, DMSO-d6): 5 ppm

2.13 (s, 3H), 2.36 (s, 3H), 2.6 (t, J = 6Hz, 2H), 2.65 (d, J = SÎTz, 3H), 3.5 (s,2H), 3.62 (s, 3H), 4.16 (t, J = 6Hz, 2H) 5.1 (d, J = 13Hz, 1H), 5.13 (s, lH),5.16(d, J = 13Hz, 1H), 7.2 (m, 1H), 7,33 (s, 5H) 7.4 - 8.3 (m,4H), 9.16 (s, 1H)

44

3380,3330,1690,

1640,1605,1530,1480, 1350, 1280,1250,1210, 1105,1050,905,830, 780, 740,700 3400, 332Ô, Í9f>0, Í740, 1690,1640,1605,1530, 1480, 1350,1280,1250,* 1210,1100, 905,830, 780,750,720

2.13 (s, 3FÍ), 2.36 (s, 3H), 2.6 (QXHzXH). 3.5 (s, 2H), 3.62 (s, 3H), 4.16 (t, J = 6Hz, 2H), 5.13 (s, 1H), 5,13 («1, J = 12Hz, 1H), 5,33 (d, J - 12Hz, 1H), 7.3- 8.3 (in, 9H), 7.33 (s, 5H), 9.2 (s, 1H)

45

46

3400,2950,174Ó, 1685, 1525,1500,1350, 1245, 1200,1190,1090, 1020, 1010,975,900, 825, 800, 760, 730, ;690 3420, f69üTíI5?, Í50Ö 1350,1210,1095,1010, 975,900,830,800 780, 760, 740

1.7 (br. s, 6H), 2.4b (s, 3H). 2.8 (br. s,'411)73.3 (s, 3H), 3,3 (m, 2H), 4.35 (m, 2H), 4.9 (s, 2H), 5.05 (s, 1H), 5.25 (br. s, 2H), 7,5-8.3 (m, 4H), 9.35 (s, !H)

T43T(^73P!XT9Ts, 311)713 -4.0 br. s, 10H), 3.77s, 3H), 4.S (m, 2H), 5.02 (d, J = 12Hz, 1H), 5.15 (s, 1H), 5.2 (d, J = 12Hz, 1H), 6.8 (br. s, 2H), 7,6-8.3 (m,4H) 9.38 (s, 1H)

47

2.45 (s, 3H), 2.9 -4717^^0^13 68^73H), 4.5 (m, 2H), 4.97 (d, J = 13Hz, 1H), 5.12 (s, 1H), 5.14 (d, J - 13Hz, 1H). 6.73 (br. s, 2H), 7.5-81 (m. 4H), 9.35 (s, 1H)

48

3450, 2960, 169Ô, 1640, 1330,1280,1210,1100, 1070,1020,910,830, 780,760,710

Pld.

sz.

Szerk. képlet

NO.

49

C2H5

C2H5

^NCH.CHjOOC

CH.

&

. COOCH

XííX

• HC1

kiterm.

olvadás

uv

a számított

pont

XMe0Hnm

%-ában

C

max,

340 mg

230

63%

—

345

CH20-C0NH2

50 (7HcC,

6HsCHyNCH2CH2OOC

CH.

NO.

■HQ

cooch2ch2oc3h7

ch2o-conh2

200 mg 71 235

41% - 72 355

Pld.

SZ.

IR (KBr): cm"*

1FI NMR (90 MHz, DMSO-d6): S ppm

49

3420, 2950, 1735, 1685, 1525, 1500, 1350, 1240, 1200,1190,1090,1020 760, 730, 690

1.19 (m, 6H), 2.45 (s, 3H), 3.06 (m, 4H). 3.25 (t, J =7Hz,2H), 3.55 (s, 3H),4.36 (t, J = 7Hz, 2H), 4.83 (s, 2H), 5,08 (,. 1H), 6.75 (br. s, 2H), 7.5—8.3 (m, 4H)

9.4 (br. s, 1H)

50

3430. 1960, 1690, 1640, 1610,1530,1480,1350, 1320. 1280, 1210, 1080, ‘>00. 830, 810, 780, 740 -700

0.8 (t, J = 8Hz, 311), 1.46 (ín, 2H), 2.4 (s. 311), 2.6 (s. 3H), 3.48 (t, J = 8Hz, 2H), 3.52 (m, 211). 3.68 (m, 2H), 4.12 ( n, 2H), 4.26 (br. s, 2H), 4,44 (m, 2H), 4,88 (d! J = 13Hz, 1H), 5,03 (s, 1 H), 5,08 (d, 1 = 13Hz, 1H), 6,65 (br. s, 2H), 7,43 (s, 5H) 7.5 - 8.2 (m,4H), 9.2 (s, 1 H)

18