Back to results
US 7,078,521 B2Granted
Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsPatrizia Minetti, Domenico Mastrojanno
Life of this patent
Estimating the term…
Abstract
A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R1H to give the corresponding enamine, which is subsequently transformed into the final compound
Claims14
A process for the preparation of formula (I) or its salt
- where:
- R is selected from the group consisting of H, Cl, Br, F, I, C1–C4 alkoxy, C1–C4 alkylthio, C1–C4 alkyl, C5–C6 cycloalkyl;
- R1 is selected from the group consisting of dialkylamine, 4-alkyl-1-piperazinyl group, 4-hydroxyalkyl-1-piperidinyl group, 1-imidazolyl group, 4-alkyl-1-piperidinyl group;
- R2 is selected from the group consisting of hydrogen, a C1–C4 alkoxy group, and a C1–C4 alkylthio group,
- by transforming a pyrrolobenzothiazepinone, substituted with the groups R and R2, into the formula (I) compound to the corresponding enamine, and optional salifying the compound with an acid.
2 more elements
A process for the preparation of formula (I) or its salt
- where:
- R is selected from the group consisting of H, Cl, Br, F, I, C1–C4 alkoxy, C1–C4 alkylthio, C1–C4 alkyl, C5–C6 cycloalkyl;
- R1 is selected from the group consisting of a dialkylamine, a 4-alkyl-1-piperazinyl group, a 4-hydroxyalkyl-1-piperazinyl group, a 1-imidazolyl group, and 4-alkyl-1-piperidinyl group;
- R2 is selected from the group consisting of hydrogen, a C1–C4 alkoxy group, and a C1–C4 alkylthio group,
- by reacting a pyrrolobenzothiazepinone of formula (Ia)
- with an amine R1H, wherein R1 is as defined above to give a compound of formula (Ib)
- which is subsequently transformed into the final compound (I), and optionally salified with an acid.
4 more elements
Dependencies are inferred from the claim text.