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翻譯,有機化學(xué),幾句話
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The incorporation of fluorinated functional groups into organic molecules has been widely recognized as a general strategy in pharmaceutical research and drug development. Fluorinated analogues of pharmaceutically relevant compounds often possess properties conducive to drug development, such as improved lipophilicity, metabolic stability, and bioavailability relative totheir nonfluorinated counterparts. Hence, the developmentof new and efficient methods for the introduction of fluorine orfluorinated moieties into organic molecules has become anintensive topic of organosynthetic chemistry. Among fluorinecontaining functional groups, the difluoromethylphosphonate group (CF2PO(OEt)2), as an in vivo stable surrogate of the phosphate group, has unique structural and electronic properties . Indeed, many CF2PO(OEt)2-containing compounds are of current interest for their use in the design and development of new drugs . For example, phosphono(diflouromethyl)- phenylalanine (F2Pmp) has shown particular utility when dealing with protein-tyrosine phosphatases (PTPs) . |

新蟲 (知名作家)
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在有機分子中引入含氟官能團(tuán)已被廣泛認(rèn)為是醫(yī)學(xué)研究和藥物開發(fā)的總體戰(zhàn)略。相較于其非氟化的同類物質(zhì),醫(yī)學(xué)相關(guān)的氟化物類似物常常有助于掌握藥物開發(fā)的性質(zhì),比如提高親油性,增強新陳代謝的穩(wěn)定性。因此,發(fā)展新的有效的向有機分子中引入氟或含氟基團(tuán)的方法已成為合成有機化學(xué)的一個熱門研究課題。在含氟官能團(tuán)中,二氟甲基磷酸二乙酯基團(tuán)(CF2PO(OEt)2)作為一個在活體中穩(wěn)定的磷酸基團(tuán)替代物,具有獨特的結(jié)構(gòu)和電子性質(zhì)。事實上,許多包含二氟甲基磷酸二乙酯基團(tuán)的化合物由于其在新藥物的設(shè)計與合成的使用而引起人們的興趣。比如,膦(二氟甲基)-苯丙氨酸(F2Pmp)在處理蛋白絡(luò)氨酸磷酸酶(PTPs)時已經(jīng)顯示出了獨特的效用。 以上是翻譯內(nèi)容,不當(dāng)之處,請多多指教! |
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