188178. lajstromszámú szabadalom • Eljárás 2-(acil-amino-mentil)-1,4-benzodiazepin-származékok előállítására

1

188 178

2

Példa

R,

r2

r3

száma

n

r4

Rs

r6

Op.°C

110.

ch3

H

0

3-thien.

3-fur.

8-CH3

H HCI

236-238

111.

ch3

H

0

4-CN-phen.

3-fur.

8-CH3

H HCI • 0,3

h2o

259-261

112.

ch3

H

0

3-CN-phen.

3-fur.

8-CH3

H HCI

193-195

113.

ch3

H

0

3-fur.

3-fur.

8-CH30

H HCI

236-239

114.

ch3

H

0

phen.

3-fur.

8-CH30

H HCI

240-242

115.

ch3

H

0

4-CF3-phen.

3-fur.

8-CH30

H HCI

240 -244

116.

ch3

H

0

4-CH3-phen.

3-fur.

H

H HCI

238-240

117.

ch3

H

0

4-CH30-phén.

3-fur.

H

H Base

Ö1

118.

ch3

H

1

2-Cl-phen.

3-fur.

8-CH30

H HCI

152-156

119.

ch3

H

0

3-fur.

3-fur.

H

H HCI

222-225

120.

ch3

H

0

4-CN-phen.

3-fur.

H

H HCI

173-178 (S)

121.

ch3

H

0

phen.

3-fur.

H

H HCI

235-237

122.

ch3

H

0

3-fur.

2-pyrid

H

H Base

143-145

123.

ch3

H

1

2-Cl-phen.

2-pyrid

H

H p-Tos • 0,3 H20

132-135

124.

ch3

H

0

4-CN-phen.

2-pyrid

H

H p-Tos ■ 0,25

h2o

201-204

125.

ch3

H

0

4-CN-phen.

3-pyrid

H

H p-Tos

199-201

126.

ch3

H

0

3-fur.

3-pyrid

H

H di-Fum

154-157

127.

ch3

H

1

2-Cl-phen.

4-pyrid.

8-CH30

H 2,25 Mai

176-178

128.

ch3

H

0

4-CN-phen.

4-pyrid.

8-CH30

H Base

Ö1

129.

ch3

H

0

3-fur.

4-pyrid.

8-CH30

H Base

Ö1

130.

ch3

H

0

phen.

2-pyrid.

7-CH3

H Base

ÖI

131.

ch3

H

0

3-fur.

2-pyrid.

7-CH3

H Base

Ö1

132.

ch3

H

0

phen.

N-CH3-2--pyrrol.

H

H p-Tos

180-182

133.

ch3

H

1

2-Cl-phen.

N-CH3-2--pyrrol.

H

H Base

135-136

134.

ch3

H

0

phen.

N-CH3-3--pyrrol.

H

H Base am

93-98

135.

ch3

H

0

phen.

3-pyrrol

H

H Base

Ö1

136.

ch3

H

0

phen.

2-thien.

7-CH30

H 1,1 HCl • 0,4 H20

202-205

137.

ch3

H

0

3-fur.

2-thien.

7-CH30

H 1,3 HCl • 0,5

h2o

143-158

138.

ch3

H

0

4-CH30-phen.

3-thien.

8-F

H Base 8-F HCl • 0,2

Ö1

139.

ch3

H

0

phen.

3,4-OCH20--phen.

3-thien.

7-CH3

H2O0,l

(CH3)2

CHOH

183-187

140.

ch3

H

0

3-thien.

7-CH3

8-F HCl

197-201

141.

ch3

H

0

3,4-0CH20--phen.

3-thien.

7-F

8-CH3HCl

212-218

142.

ch3

H

0

4-OH-phen.

3-thien.

7-CH30

H 1,1 HCl • 0,1

h2o

193-197

143.

ch3

H

0

4-CH3COO-phen.

3-thien.

7-CH30

H Base

Ö1

144.

ch3

H

0

4-NH2-phen.

3-thien.

7-C1

H 1,85 HCl • 0,5 H20, am

112-116

145.

ch3

H

0

4-CH3CONH-phen.

3-thien.

7-C1

H 1,05 HCl • 0,25 H20

178-182

146.

ch3

H

0

4-(CH3)2N-phen.

3-thien.

7-CI

H 1,9 HCl • 0,45 H20, am

122-128

147.

ch3

H

1

4-F-phen.

3-thien.

H

H HCl

223-229

148.

ch3

H

1

2-F-phen.

3-thien.

H

H HCl

198-200

149.

ch3

H

1

2-F-phen.

3-thien.

7,8-OCH20

HCl

227-234

150.

ch3

H

0

phen.

N-CH3-3

pyrrol.

8-OCH3

H Base

Ö1

14