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химия и технология химико- фармацевтических препаратов

химия и технология химико- фармацевтических препаратов

химия и технология химико- фармацевтических препаратов

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3.7. Препараты на основе фенот<strong>и</strong>аз<strong>и</strong>на. Ам<strong>и</strong>наз<strong>и</strong>н.<br />

CI<br />

CH 3<br />

CI<br />

HNO 3 , 57%<br />

130-135 0 С; CI<br />

p=0.6-0.8 МПа;<br />

7-8 час.<br />

COOH<br />

CI<br />

H 2 NPh, KCO 3 ,<br />

Cu<br />

102-109 0 C;<br />

6 час.<br />

HOOC<br />

N<br />

H<br />

CI<br />

180-200 0 С<br />

перегонка<br />

в гл.вак.<br />

- СO 2<br />

N<br />

H<br />

CI<br />

S, I 2<br />

170-180 0 C<br />

-H 2 S<br />

S<br />

N<br />

H<br />

CI<br />

CI(CH 2 ) 3 NMe 2<br />

S<br />

-<br />

NaOH<br />

-NaCI,-H 2 O<br />

N<br />

(CH 2 ) 3 NMe<br />

HCI<br />

CI<br />

S<br />

N<br />

(CH 2 ) 3 NMe<br />

.<br />

CI<br />

HCI<br />

ам<strong>и</strong>наз<strong>и</strong>н<br />

Этапераз<strong>и</strong>н.<br />

PhCI; PhMe<br />

H 2 , Ni; сп<strong>и</strong>рт<br />

H 2 CO,HCOOH SOCI 2 , к<strong>и</strong>п.<br />

HO CH 2 CH 2 C N<br />

HO CH<br />

t=95-100 0 2 CH 2 СH 2 NH 2 HO CH2 CH 2 СH 2 NMe 2 CI CH 2 CH 2 СH 2 NMe 2<br />

C;<br />

- SO 2 ,-<br />

HCI<br />

p=2.0-2.2 МПА<br />

CH 2<br />

O<br />

CH 2<br />

HN<br />

NH<br />

. 6 H 2 O<br />

MeOH<br />

t=70 0 С<br />

HN N (CH 2 ) 2 OH<br />

CICH 2 CH 2 CH 2 Br<br />

PhMe,70-80 0 C<br />

CICH 2 CH 2 CH 2 N<br />

N<br />

(CH 2 ) 2 OH.<br />

HBr<br />

S<br />

S<br />

.<br />

2HCI<br />

N<br />

H<br />

CI<br />

1)NaOH;<br />

2)HCI<br />

N<br />

CI<br />

CH 2 CH 2 CH 2 N<br />

N (CH 2 ) 2 OH этапераз<strong>и</strong>н<br />

- NaBr, - NaCI<br />

Тр<strong>и</strong>фтаз<strong>и</strong>н.<br />

HNO 3 ,<br />

H 2 SO 4<br />

CF 3<br />

40-50 0 C<br />

NO 2<br />

CF 3 [H]<br />

H 2 O,к<strong>и</strong>п<br />

NH 2<br />

CF 3<br />

Ac 2 O<br />

CF 3<br />

NHCOCH 3<br />

Br<br />

H 2 O,<br />

, CuBr,Cu,<br />

HCI<br />

к<strong>и</strong>п.<br />

к<strong>и</strong>п.<br />

- HBr<br />

N CF 3<br />

COCH 3<br />

N CF 3<br />

H<br />

S, I 2<br />

S<br />

CICH 2 CH 2 CH 2 Br<br />

S<br />

N CH 3<br />

0<br />

145-155 C,<br />

-<br />

N CF<br />

HBr<br />

90-100 0 C<br />

3<br />

N CF<br />

N CF 3<br />

3<br />

-H 2 S<br />

H<br />

CH 2 CH 2 CH 2 CI<br />

CH 2 CH 2 CH 2 N N CH 3<br />

Me 2 NCH 2 CH 2 OH + SOCI 2 Me 2 NCH 2 CH 2 CI . HCI + SO 2<br />

HN<br />

S<br />

тр<strong>и</strong>фтаз<strong>и</strong>н<br />

Эт<strong>и</strong>з<strong>и</strong>н.<br />

S<br />

N<br />

H<br />

S<br />

PhMe<br />

+ Me 2 NCH 2 CH 2 CI . HCI + 2NaOH тв.<br />

-2NaOH,-2H 2 O N<br />

CH 2 CH 2 NMe 2<br />

С 2 H 5 OH,<br />

HCI 36%<br />

S<br />

.<br />

HCI<br />

N<br />

CH 2 CH 2 NMe 2<br />

эт<strong>и</strong>з<strong>и</strong>н<br />

28

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