Direct Synthesis of Polylactide (PLA)-Chlorphenesin Prodrug and Optimization Thereof with the Aid of DOE,Organic Process Research & Development

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Direct Synthesis of Polylactide (PLA)-Chlorphenesin Prodrug and Optimization Thereof with the Aid of DOE
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-12-08 00:00:00 , DOI: 10.1021/acs.oprd.7b00266
Agnieszka Sebai ₁ , Paweł Ruśkowski ₁ , Vanessa Bijak ₁ , Agnieszka Gadomska-Gajadhur ₁ , Aleksandra Kruk ₁ , Ludwik Synoradzki ₁

Affiliation

A direct, one-pot, solvent-free method for preparation of macromolecular prodrug composed of chlorphenesin (CF, 1) and polylactide (2) was developed. The procedure involves addition of chlorphenesin to l-lactide followed by ring-opening polymerization of the latter. The process was optimized by factorial design to maximize the conversion and to obtain sufficiently high average molecular mass of the prodrug. Proposed mathematical model allows the length of the polymeric chain to be controlled, influencing the duration of the therapeutic effect.

中文翻译：

聚乳酸（PLA）-氯酚前体药物的直接合成及其在DOE的帮助下优化

开发了一种直接，一锅，无溶剂的方法来制备由氯酚素（CF，1）和聚丙交酯（2）组成的大分子前药。该方法包括将氯酚素加到1-丙交酯中，然后将后者开环聚合。该过程通过析因设计进行了优化，以最大程度地提高转化率并获得足够高的前药平均分子量。提出的数学模型可以控制聚合物链的长度，从而影响治疗效果的持续时间。

更新日期：2017-12-08

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