PURPOSE: To obtain a new azaspiro derivative useful as an intermediate for producing a quinolonecarboxylic acid derivative having strongly antimicrobial activity in a wide spectrum.
CONSTITUTION: This compound is shown by formula I [R1 is H, a (substituted) 1-20C alkyl, a (substituted) benzyl or a nitrogen-protecting group; R2 is H or CH3; R3 is CO2H, CON3, NCO, etc.; a carbon atom to which R3 is bonded is a chiral carbon atom and is a stereochemical configuration of (1,3)-R,S,(1,3)-R, R,(1,3)-S,S or (1,3)-S,R; (n) is 1 or 2] or its salt such as 1-amino-5- azaspiro[2,4]heptane. The compound of formula I in which R3 is CO2H is obtained by reacting a compound of formula II with a compound of the formula P(C6H5) 3CH2-CO2R8.X (R8 is a 1-5C alkyl; X is I or Br) in the presence of a strong base to give a compound of formula III, reacting the compound with methylene chloride and titanium chloride to give a compound of formula IV, hydrolyzing the compound and acidifying the reaction product with an acid.
| JP2012506883 | Substituted spiroamine |
| JPH06508378 | INDUSTRIAL APPLICABILITY INDUSTRIAL APPLICABILITY- and imidealkyl-piperazines |
| WO/2020/132653 | HETEROARYL AMIDES USEFUL AS KIF18A INHIBITORS |
BOKU MEIKAN
KAWA ZAITO
HAKU KEIGIYOU
