(1R,4S)-4-Hydroxycyclopent-2-en-1-yl acetate is a chiral small building block that was requested to advance several Pfizer programs into the clinic. Pfizer and Syncom partnered to develop a photo-oxidation process of cyclopentadiene using a flow approach followed by subsequent bis-acetylation of the meso diol and final biocatalytic desymmetrization. This continuous process was demonstrated on a 6 g·h^–1 input and is amenable to larger scale. The optimization and scale-up of this sequence is described therein.

中文翻译：

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连续工艺对环戊二烯的光氧化作用：在合成（1 R，4 S）-4-羟基环戊-2-烯-1-基乙酸酯中的应用

（1 R，4 S）-4-羟基环戊-2-en-1-基乙酸盐是一种手性小分子砌块，被要求将一些辉瑞计划推进临床。辉瑞公司和Syncom公司合作开发了一种使用流动方法的环戊二烯光氧化工艺，随后进行了内消旋二醇的双乙酰化和最终的生物催化脱对称。此连续过程在6 g·h ^–1的输入量下得到了证明，并且可以进行较大规模的应用。其中描述了该序列的优化和放大。