Preparing 1-(hydroxymethyl)-triazolobenzodiazepines and 1-(amino

Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal

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2602433, 2602444, C07D48704

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active

045016984

ABSTRACT:
A process is provided for converting 1-hydrogen-triazolo[4,3-a]-[1,4]benzodiazepines, e.g., estazolam, to 1-(hydroxymethyl)-triazolo-[4,3-a][1,4]benzodiazepines, and, if desired, these 1-(hydroxymethyl)-compounds to 1-aminomethyl compounds, e.g., to adinazolam, without the need for column chromatography or sealed tube procedures, and while minimizing 1,4-bis-(hydroxymethyl)- group formation.

REFERENCES:
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patent: 3914245 (1975-10-01), Gall
patent: 3947466 (1976-03-01), Gall et al.
patent: 3992393 (1976-11-01), Gall
patent: 3994941 (1976-11-01), Hester
patent: 3995043 (1976-11-01), Hester, Jr.
patent: 4001262 (1977-01-01), Gall
patent: 4250094 (1981-02-01), Hester, Jr.
Derwent Abstract 70853W/43 of CH 567-023 dated Sep. 30, 1975.
Derwent Abstract 70854W/43 of CH 567-024 dated Sep. 30, 1975.
Derwent Abstract 75881W/46 of CH 568-319 dated Oct. 31, 1975.
Derwent Abstract 35430T-B of Belgian 775558-Q dated May 19, 1972.
Derwent Abstract 48681A/27 of Japanese Patent Publ. No. J5 3059-696.
Derwent Abstract 52339T-B of W. German DT-2201210-C.
Derwent Abstract 40575T-B of Belgian App. No. 776514-Q.

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