Heterocyclic Chemistry at a Glance

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142 Heterocycles with More than Two Heteroatoms: Higher Azoles (5-Membered) and Higher Azines (6-Membered)


Dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate, which is much used in Diels–Alder reactions, is prepared by the base-
catalysed dimerisation of ethyl diazoacetate, then oxidation of the resulting dihydro-tetrazine (after re-esterifi cation).


Exercises



  1. What are the products of the following (Diels–Alder) reactions:
    (i) 1-pyrrolidinylcyclopentene with (a) 1,3,5-triazine and (b) 1,2,4-triazine;
    (ii) 3-phenyl-1,2,4,5-tetrazine with 1,1-diethoxyethene?

  2. Thiophosgene (S=CCl 2 ) reacts at low temperature with sodium azide to give a product that contains no
    azide group; on subsequent reaction with methylamine this compound is converted into C 2 H 4 N 4 S – what
    are the structures?

  3. What are the products of the reaction of PhCONH 2 with DMFDMA to give C 10 H 12 N 2 O and then this with
    (a) N 2 H 4 or (b) H 2 NOH?

  4. 1,3,5-Triazine reacts with
    (i) aminoguanidine [H 2 NN=C(NH 2 ) 2 ] to give 2-amino-1,3,4-triazole and with
    (ii) diethyl malonate to give ethyl 4-hydroxypyrimidine 5-carboxylate. What reasonable mechanistic
    sequences will rationalise these transformations?

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