Pyrrolo benzothiazepin-7 ones

Formylation of 5H-benzo[/]pyrrolo[l,2-d][l,4]diazepin-6(7H)-one 180 pyrrole ring with POCI3/DMF is known (Scheme 36, Section 3.1.1.1 (1992BMCL1639)). Formyation of pyrrolo-benzothiazepine can be accomplished using POCI3/ PhNMeCHO (Scheme 76 (2004JMC143)). The monoaldehyde 375 (R = H) is... 

Benzo[e]thieno[3,2- ]thiepin-10(5Ef)-one 388 can be smoothly reduced with sodium borohydride to the corresponding alcohol, which forms the chloro substituted compound under standard treatment with thionyl chloride (1991CPB2564). Dihydro derivatives of pyrrolo-benzothiazepine 377 have been reported starting from ketone 373 by a carbonyl reduction, bromination and amination sequence (Scheme 76, Section 5.1.1 (1998JMC3763, 2002JMC344, 2004JMC143)). 

Pyrrolo[3,4-c][l,5]-benzothiazepin-3-ones 300 are available from ketoester 299 by a three-step sequence which includes hydrolysis and decarboxylation, aldol condensation and cyclization with o-aminothiophenol (Equation (35) (1993CE773)). 

Dimethyl-2,3,4,10-tetrahydro-l//-pyrrolo[3,4-c][l,5]benzothiazepin-1-ones (10) were prepared by a reaction between 2-aminothiophenol (5) and 3-arylmethylene-5,5-dimethyltetramic acids (9) in 81-%% yields (Scheme 4) (84YZ1004). 

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