FIELD: chemical or physical processes.
SUBSTANCE: invention relates to a method of producing a pyrrolopyridine derivative of formula I, involving: (S-1) obtaining a compound of formula 3 by cyclisation of a compound of formula 1, a butane derivative of formula 2 and 4-chlorobenzoylacetonitrile at temperature of 30–60 °C; (S-2) obtaining a compound of formula 4 by cyclisation of compound of formula 3 and an acetyl pyruvate derivative at temperature of 40–80 °C; (S-3) obtaining a compound of formula 5 from a compound of formula 4 by chiral reduction at a temperature of −10–10 °C; (S-4) obtaining a compound of formula 6 from a compound of formula 5 by alkylation at a temperature of −5–30 °C; (S-5) obtaining a compound of formula I from a compound of formula 6 by hydrolysis at temperature of 20–80 °C; where X is Cl, Br or I and R is C1–4alkyl. Invention also relates to compounds of formula 3, 4 and 5, where R is C1–4alkyl.
EFFECT: method of producing a pyrrolopyridine derivative of formula I with high purity and high output.
13 cl, 7 ex
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Authors
Dates
2024-11-22—Published
2021-01-11—Filed