Translated Title

Advances in the Synthesis of Venetoclax as a New Drug for the Treatment of Chronic Lymphocytic Leukemia

Translated Abstract

Venetoclax,the　first　selective　inhibitor　of　B-cell　lymphoma-2,was　approved　by　FDA　for　treating　relapsed　or　refractory　chronic　lymphocytic　leukemia　patients　with　17p　deletion　who　have　received　at　least　one　prior　therapy.In　this　paper,four　reported　synthesis　routes　of　Venetoclax　are　reviewed.The　comparison　and　analysis　of　these　synthesis　routes　showed　that　convergent　strategies　are　often　applied　in　the　synthesis　of　Venetoclax,and　it　includes　the　synthesis　of　four　kinds　of　key　intermediates.The　synthesis　routes　of　Venetoclax　are　continuously　improved　in　these　respects　of　using　cheap　and　readily　available　raw　materials,raw　materials　or　synthesis　approaches　with　higher　reaction　selectivity,milder　reaction　conditions　and　enhancing　gross　yields.In　view　of　the　fact　that　all　of　the　four　synthesis　routes　involve　precious　metal　(palladium)　and　ligands　as　catalysts,investigation　of　polymersupported　palladium　and　ligands　as　catalysts　will　simplify　the　recovery　of　catalysts　and　separation　process,and　further　decrease　the　preparation　cost.This　also　helps　to　the　development　of　sustainable　industrial　production　of　Venetoclax.If　this　improvement　is　accomplished,the　fourth　synthesis　route　of　Venetoclax　has　the　greatest　potential　for　industrialization.

Translated Keyword

Chronic lymphocytic leukemia
Synthesis
Venetoclax

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Type

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Project No.

Access Number

WF:perioarticalhxtb2201802003

Language

Chinese

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