Patent ID: 11873316
Assignee: WAVE LIFE SCIENCES LTD.
Field: Organic fine chemistry (Chemistry)
Classification: CPC C | IPC C

Claim 0:
1. A method for preparing a phosphoramidite, comprising steps of:
a) providing a preparation comprising a phosphoramidite product and one or more reaction byproducts of the synthesis of the phosphoramidite; and
b) performing a filtration step on the preparation to provide a filtrate, wherein the filtrate contains a reduced level of the one or more reaction byproducts relative to the product as compared to that level present in the preparation prior to the filtration step,
wherein:
after the phosphoramidite product is formed, no solution comprising the phosphoramidite product is contacted with water of more than 100 mole equivalents of the phosphoramidite; and
the phosphoramidite has the structure of formula I:, wherein:
BA is, wherein R is hydrogen or optionally substituted C1-6 aliphatic;
SU is, R5s is R′ or —OR′;
wherein:
(1) R2s is —F or —OCH2CH2OMe, and, or
(2) R2s is —F, —H, or —OCH2CH2OMe, and, each R′ is independently —R, —C(O)R, —CO2R, or —SO2R, or:
two or more R′ are taken together with their intervening atoms to form an optionally substituted monocyclic, bicyclic or polycyclic, saturated, partially unsaturated, or aryl 3-30 membered ring having, in addition to the intervening atoms, 0-10 heteroatoms independently selected from oxygen, nitrogen, sulfur, phosphorus and silicon; and

each R is independently hydrogen, or an optionally substituted group selected from C1-30 aliphatic, C1-30 heteroaliphatic having 1-10 heteroatoms independently selected from oxygen, nitrogen, sulfur, phosphorus and silicon, C6-30 aryl, a 5-30 membered heteroaryl ring having 1-10 heteroatoms independently selected from oxygen, nitrogen, sulfur, phosphorus and silicon, and a 3-30 membered heterocyclic ring having 1-10 heteroatoms independently selected from oxygen, nitrogen, sulfur, phosphorus and silicon.