Process for preparing azetidine derivatives and intermediates th

Details Process for preparing azetidine derivatives and intermediates th Process for preparing azetidine derivatives and intermediates th

1985-06-12

1987-05-12

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548950, C07D20504

Patent

active

046651977

ABSTRACT:
The invention provides a process for preparing azetidine-3-carboxylic acid or salts thereof; useful as chemical hybridizing agents, which comprises treating a compound of the formula ##STR1## wherein R represents a hydrogen atom or a group of formula R.sup.1 R.sup.2 CH-- wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl or optionally substituted phenyl moieties, with nitric acid and subjecting the resulting initial product to acid conditions to produce an acid-addition salt of azetidine-3-carboxylic acid, and thereafter, if desired, converting the acid-addition salt to the free acid or another salt of the acid, 1-nitrosoazetidine-3,3-dicarboxylic acid, 1-nitrosoazetidine-3-carboxylic acid and salts thereof being intermediates in the process.

REFERENCES:
patent: 4569795 (1986-02-01), Scholes et al.
Nagasawa, et al., J. Med. Chem., vol. 16(5), (1973), pp. 583-585.
March, ed., Advanced Organic Chemistry, 2nd ed., (1977), McGraw-Hill, New York, pp. 569-572, 1107-1108.

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