A mild and efficient THP protection of indazoles and benzyl alcohols in water |
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Authors: | Yang Zhan Xiao Ding Hailong Wang Haihua Yu Feng Ren |
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Institution: | Neurodegeneration DPU, Neurosciences Therapeutic Area Unit, GSK Pharmaceuticals R&D, 898 Halei Road, Zhangjiang Hi-Tech Park, Pudong, Shanghai 201203, PR China |
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Abstract: | A mild and efficient method for THP protection of indazoles and benzyl alcohols has been developed in water, the most environmentally friendly solvent, in which Tween 20 (2% w/w) was added to form aqueous micelles to increase the solubility of starting materials. This aqueous protocol allowed the reaction to proceed smoothly at room temperature and with only 1.2 equiv of DHP, providing moderate to good yields of THP protected products for a wide scope of substrates. In addition, the methodology was highly practical in the large-scale synthesis (1?g synthesis of 2c as an example), wherein the convenient work-up and purification procedure (simple filtration) made the protocol even more attractive. |
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Keywords: | Indazoles Benzyl alcohols THP protection Aqueous micelles Tween 20 |
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