4-Chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide → (R)-2-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-4-ylamino}-3-furan-3-yl-propan-1-ol

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Reaction Steps

Starting from 4-chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide (cf Example 124, 3.1.3) and (R)-2-amino-3-furan-3-yl-propan-1-ol trifluoroacetate, the two diastereomers of (R)-2-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5λ4-thieno[3,2-d]pyrimidin-4-ylamino}-3-furan-3-yl-propan-1-ol are prepared as described in Example 124 (cf 3.1.4). The diastereomers are separated by preparative HPLC (method B). Analytical HPLC-MS (method D): Diastereomer 1: RT=1.23 min (Example 206); Diastereomer 2: RT=1.24 min (Example 207).

Provenance & Evidence