Processes and intermediates useful in the preparation of flutrol

Details Processes and intermediates useful in the preparation of flutrol Processes and intermediates useful in the preparation of flutrol

1982-09-30

1984-10-16

Rotman, Alan L.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546 86, 546 87, 424256, C07D47104, A61K 31445

Patent

active

044776691

ABSTRACT:
1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4, 3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyl)]-2,3,4,5 -tetrahydro-1H-pyrido[4,3-b]indole (flutroline) or to 8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (an alternative flutroline intermediate).

REFERENCES:
patent: 4001263 (1977-01-01), Plattner et al.
patent: 4014890 (1970-03-01), Welch
patent: 4224329 (1980-09-01), Welch
patent: 4267331 (1981-05-01), Welch
Rylander, "Catalytic Hydrogenation over Platinum Metals," pp. 291-303, Academic Press, (1967).
Harbert et al., J. Med. Chem. 23, pp. 635-643 (1980).
Murakami et al., Heterocycles 12, pp. 1571-1574, (1979).

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