238 Synthetic Routes toN-Nitro
+ 4 CH 2 O + H 2 N(CH 2 )nNH 2
N
N
N
N
N
2 )nN(CH
NO 2
NO 2 NO 2
NO 2
HNO 3 , Ac 2 O
50–60 °C
205, n = 2
206, n = 3
2
NHNO 2
2
NHNO 2
AcO
NO 2
NO 2 NO 2
203, n = 2
204, n = 3
(CH 2 )n
2
N N N
Figure 5.85
(204) are formed when the amine components are ethylenediamine and 1,3-diaminopropane
respectively.^161 Nitrolysis of the bicycles (203) and (204) with nitric acid in acetic anhydride
yields the linear diacetates (205) and (206), respectively.^161 Note that only bicycle (193), where
the triazacycloheptane units are separated by a single methylene group, leads to 1,3,5-trinitro-
1,3,5-triazacycloheptane (194) on nitrolysis. 1,3,5-Trinitro-1,3,5-triazacycloheptane (194) has
never been isolated from the nitrolysis of extended bicycles like (203) and (204).
NO 2
2 N CO
O 2 N
O 2 N
NO 2
CH 2 OH
NH 4 OAc (aq) NO^2
C
NO 2
CH 2 NHCH 2 C
NO 2
NO 2
NO 2
NO 2
C
NO 2
CH 2 NCH 2 C
NO 2
NO 2
NO 2
NO 2
HNO 3
207
208
209
84 %
Figure 5.86
The use of primary nitramines in Mannich reactions is an important route to numerous
secondary nitramines. However, a far more common route to such nitramines involves the
Mannich condensation of a terminalgem-dinitroalkane, formaldehyde, and an amine, followed
byN-nitration of the resulting polynitroalkylamine.^162 The preformed methylol derivative of
thegem-dinitroalkane is often used in these reactions and so formaldehyde can be omitted.
This route has been used to synthesize explosives like (92)^163 and (209).^164
NH 4 OAc (aq)
40–50 °C
N
H
NO 2
O 2 N NO 2
O 2 N
N
NO 2
O 2 N NO 2
O 2 N
NO 2
HNO 3 , Ac 2 O
47 %
210
C
211
92
CCH 2
NO 2
NO 2
NO 2
NO 2
HOCH 2 CH 2 OH
54 %
Figure 5.87