| 主权项 |
1. A process for preparation of Lubiprostone comprising hydrogenation, in the presence of a suitable hydrogenation catalyst, of a compound of Formula 10: wherein R1, R2 and R3 are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, and substituted arylalkyl; at least one of R1, R2 and R3 is aryl or substituted aryl; R6 is H or C(R1′)(R2′)(R3′); R1′, R2′ and R3′ are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, and substituted arylalkyl; and at least one of R1′, R2′ and R3′ is aryl or substituted aryl; S/D is a single or a double bond; wherein
alkyl refers to a straight chain, branched chain or cyclic alkyl group of 1 to 10 carbon atoms, that may be fully saturated, mono- or polyunsaturated;aryl refers to a polyunsaturated, aromatic hydrocarbon of from 1 to 3 rings that are either fused or covalently linked, optionally containing from 1 to 4 heteroatoms selected from N, O and S, wherein the nitrogen and sulphur atoms are optionally oxidized, and the nitrogen atom is optionally quaternized;arylalkyl refers to groups in which an aryl group is attached to an alkyl group, optionally where a methylene carbon of the alkyl group is replaced by an oxygen atom; andthe substitution of the alkyl, aryl or arylalkyl group refers to the presence of one or more substituents selected from the group consisting alkyl or alkoxy of from 1 to 10 carbons, halogen, NO2 and trifluoromethyl. |
