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OwnerAndres Francesch, Carolina Fernandez +8inventors
InventorsAndres Francesch, Carolina Fernandez, Jose Luis Chicharro, Pilar Gallego, Maria Zarzuelo, Ignacio Manzanares, Marta Perez, Carmen Cuevas, Maria Jesus Martin, Simon Munt
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Processes are provided for preparing compounds with a fused ring structure of formula (XIV). Such products include ecteinascidins and have a spiroamine-1,4-bridge. The process involving forming a 1,4 bridge using a 1-labile, 10-hydroxy, 18-protected hydroxy, di-6,8-en-5-one fused ring compound. After formation of the 1,4 bridge, C-18 protection is removed before spiroamine introduction. 1
A process for preparing an ecteinascidin product with a spiroamine-1,4-bridge, the process involving forming a 1,4 bridge using a 1-labile, 10-hydroxy, 18-protected hydroxy, di-6,8-en-5-one fused ring compound, wherein C-18 protection is removed before spiroamine introduction.
A process according to any preceding claim, wherein the 18-protected group of the 1-labile, 10-hydroxy, 18-protected hydroxy, di-6,8-en-5-one fused ring compound is protected with:
A process according to any preceding claim, wherein the 1-labile group is an N-protected cysteinyloxymethylene group of the formula
A process according to any preceding claim, which starts from a 1-aminomethylene, 5-protected hydroxy, 7,8-dioxymethylene, 18-hydroxy, 21-cyano fused ring compound
A process according to any preceding claim, wherein the product is of formula (XXIIb):
A process according to any preceding claim, wherein the ecteinascidin product is ecteinascidin 743.
A process step in the manufacture of an ecteinascidin comopund, the step comprising removing both protecting groups in a single step, in accordance with the following scheme:
Dependencies are inferred from the claim text.