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A series of polylactic acid (PLA) conjugates (PLA‐ES) are synthesized via direct melt polycondensation (DMP) of lactic acid (LA) with ethisterone (ES) in the presence of 0.3 wt% toluenesulfonic acid at 160 °C for 6 h. The drug content of PLA conjugates can be simply adjustable. Further functionalization via Click chemistry is also achieved to extend the biomedicine application of biopolymer based drug delivery.

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MTT tests of 2(5H)-furanone derivatives obtained via metal-free C–N coupling show that amino acids as linkers have no toxic effect.