单体和配体
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Amidite 合成
我们的团队拥有丰富的经验，合成过 1,000 多种结构颇具挑战的定制 Amidite 分⼦，有力⽀持您的寡核苷酸发现项⽬。此外，我们还提供 500 余种 Amidite ⽬录产品。
我们在 Amidite 修饰方面经验丰富：
- 2'/3'/4' 修饰，含 GalNAc 基团、脂质、胺基、炔基
- 糖骨架修饰：双环糖、氮杂/硫代糖、⽆环糖
- 碱基修饰：7-脱氮腺嘌呤/鸟嘌呤 (7-deaza A/G)、伪尿苷 (pU)、N-甲基伪尿苷 (N-Me pU)
- 治疗性 RNA 修饰：2’-O-甲基 (2’-OMe)、2’-氟 (2’-F)、2’-O-甲氧基乙基 (2’-O-MOE)
- 磷骨架修饰：PACE、硫代亚磷酰胺 (thiophosphoramidite)、甲基磷酸酯 (MeP)、乙基磷酸酯 (EtP)
- 碱基保护替代品：苯甲酰基 (Bz)、乙酰基 (Ac)、异丁酰基 (iBu)、对羟基苯甲酰基 (pac/iPr-pac)、O-NPE 等
- 功能/偶联修饰剂：磷酸酯试剂、氨基和硫醇连接子、间隔物、胆固醇、染料等
Sample Amidite Molecules
RNAi-Amidite
(2′-F, OMe Moe, OTBS, etc.)
LNA Amidite
TNA Amidite
Vpm-POM
DNA C(Bz) Amidite
PACE Amidite
Thio-Amidite
PMO Monomer
GalNAc 合成
N-乙酰半乳糖胺 (GalNAc) 是半乳糖的氨基糖衍生物。与 GalNAc 偶联是增强 siRNA 靶器官积累和促进细胞吸收的有效方法。
我们的团队在合成 100 多种 GalNAc 分子方面拥有丰富的经验，包括单-GalNAc 、三-GalNAc 、四-GalNAc 、GalNAc 酰胺、 GalNAc PFP 酯、GalNAc N3和 GalNAc-PEG 偶联物等。
我们拥有超过 100 种 GalNAc 构建单元和 CPG/PS 偶联树脂，可加速您的 GalNAc-寡核苷酸药物发现项目 。
Overcome GalNAc synthesis challenges
There are many synthetic challenges for GalNAc because most of the intermediates are oily or foamy solids. The synthesis involves many columns and prep-HPLC purification steps, resulting scale-up difficulties and low yields. Analytical method for GalNAc synthesis is also challenging due to low UV response, complex impurity profile and poor stability.
Original Process
Oil Intermediates
Modified Process
Solid Intermediates
Enabled by strong chemistry platform, WuXi TIDES developed convergent routes through telescoping processes without column purification steps. The isolated intermediates were stable solids. We applied the precipitation process and/or spray drying process to reduce the needs for the columns and prep-HPLC steps. Our analytical teams identified many GalNAc-related impurities to support method development and release testing.
