FREMGANGSMAADE TIL FREMSTILLING AF BENZISOXAZOLDERIVATER

2-Cyclic amino-2-[1,2-benzisoxazol-3-yl]acetic acid derivatives of the formula: …… (wherein R1 is hydrogen or a halogen atom, R2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the piperidine moiety is attached at its...

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Bibliographic Details
Main Authors KADOKAWA TOSHIAKI, MIZUTA HIROYUKI, NARUTO SHUNSUKE, KAWASHIMA KATSUYOSHI, NISHIMURA HARUKI
Format Patent
LanguageDanish
Published 27.02.1983
Edition3
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
LAND VEHICLES FOR TRAVELLING OTHERWISE THAN ON RAILS
MEDICAL OR VETERINARY SCIENCE
METALLURGY
MOTOR VEHICLES
ORGANIC CHEMISTRY
PERFORMING OPERATIONS
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
TRAILERS
TRANSPORTING
VEHICLE SUSPENSION ARRANGEMENTS
VEHICLES IN GENERAL
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Summary:2-Cyclic amino-2-[1,2-benzisoxazol-3-yl]acetic acid derivatives of the formula: …… (wherein R1 is hydrogen or a halogen atom, R2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the piperidine moiety is attached at its 3- or 4-position), and their pharmaceutically acceptable acid addition salts and quaternary ammonium salts have potent anticholinergic antispasmodic activity, while they are weak in side effects such as mydriasis, inhibition of salivary secretion and tachycardia. The preferred compounds are …… and the 1-ethyl-1-methyl piperidinium iodide derivative thereof. … Compounds (I) may be made from Am-H and a 2-haloacetic acid derivative (whose synthesis is described). They can be selectively quaternised at the piperidine N-atom.
Bibliography:Application Number: DK19820003758