[NH2:1][C@@H:2]1[C:10]2[C:5](=[CH:6][CH:7]=[CH:8][CH:9]=2)[CH2:4][C@@H:3]1[OH:11].C(Cl)Cl.C(N(CC)CC)C.[CH3:22][S:23](Cl)(=[O:25])=[O:24]>O>[CH3:22][S:23]([O:11][C@H:3]1[CH2:4][C:5]2[C:10](=[CH:9][CH:8]=[CH:7][CH:6]=2)[C@H:2]1[NH:1][S:23]([CH3:22])(=[O:25])=[O:24])(=[O:25])=[O:24](1R,2S)-1-amino-2-indanol (300 mg, 2.01 mmol) is in suspended 10 mL DCM, combined with triethylamine (1.68 mL, 12.1 mmol) and cooled to 0° C. Then methanesulphonic acid chloride (467 μL, 6.03 mmol) is added dropwise and the reaction mixture is left to warm up to RT. The reaction mixture is stirred for 1 h at RT and once the reaction is complete it is mixed with water and extracted with DCM. The organic phase is dried on MgSO4, filtered, the filtrate is evaporated down and the crude product B-1a (HPLC-MS: tRet.=1.03 min; MS (m-H)−=304) is used in the subsequent reactions without further purification.
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