186593-56-6Relevant articles and documents
AZETIDOBENZODIAZEPINE DIMERS AND CONJUGATES COMPRISING THEM FOR USE IN THE TREATMENT OF CANCER
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, (2020/10/09)
A compound of formula IV: as well as drug-linkers and conjugates comprising this compound, and the use of the conjugates in treating cancer.
Synthesis of a new precursor to the nicotinic receptor tracer 5-IA-85380 precursor using trimethylsilyl iodide as deblocking agent
Brenner, Eric,Baldwin, Ronald M.,Tamagnan, Gilles
, p. 3607 - 3610 (2007/10/03)
We describe the synthesis of a new precursor of 5-IA-85380, specific radiotracer for α4β2 nicotinic acetylcholine receptors. (S)-5-Trimethylstannyl-3-(2-azetidinylmethoxy)pyridine (4) was prepared in six steps and 62% overall yield starting from (S)-2- azetidinecarboxylic acid. The key step of this synthesis is selective release of the amine function without removing the stannyl moiety using trimethylsilyl iodine.
Processes for producing azetidine-2-carboxylic acid and intermediates thereof
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, (2008/06/13)
PCT No. PCT/JP98/01895 Sec. 371 Date Dec. 30, 1999 Sec. 102(e) Date Dec. 30, 1999 PCT Filed Apr. 24, 1998 PCT Pub. No. WO98/47867 PCT Pub. Date Oct. 29, 1998The present invention has its object to provide a process for producing azetidine-2-carboxylic acid and an intermediate thereof, which is efficient and economical and suited for industrial practice. The present invention is related to a process for producing azetidine-2-carboxylic acid of the following formula (5), which comprises subjecting a 4-oxo-2-azetidinecarboxylic acid derivative represented by the general formula (1) to hydride reduction to give azetidine-2-methanol of the following formula (2), treating the same with an amino-protecting agent to give N-protected azetidine-2-methanol represented by the following general formula (3), treating this with an oxidizing agent to give N-protected azetidine-2-carboxylic acid represented by the following general formula (4) and, further, subjecting the amino-protecting group thereof to elimination.