《Synthesis, Stability, and Biological Studies of Fluorinated Analogues of Thromboxane A2》 was written by Jing, Changcheng; Mallah, Shahida; Kriemen, Ella; Bennett, Steven H.; Fasano, Valerio; Lennox, Alastair J. J.; Hers, Ingeborg; Aggarwal, Varinder K.. Reference of 2,5-DimethoxytetrahydrofuranThis research focused onthromboxane A2 fluorinated preparation platelet aggregation induction; hydrolysis kinetics fluorinated thromboxane A2. The article conveys some information:
Platelet activation results in the generation of thromboxane A2 (TxA2), which promotes thrombus formation by further amplifying platelet function, as well as causing vasoconstriction. Due to its role in thrombus formation and cardiovascular disease, its production is the target of antiplatelet drugs such as aspirin. However, the study of TxA2-stimulated cellular function has been limited by its instability (t1/2 = 32 s, pH = 7.4). Although more stable analogs such as U46619 and difluorinated 10,10-F2-TxA2 have been prepared, we targeted a closer mimic to TxA2 itself, monofluorinated 10-F-TxA2, since the number of fluorine atoms can affect function. Key steps in the synthesis of F-TxA2 included α-fluorination of a lactone bearing a β-alkoxy group, and a novel synthesis of the strained acetal. F-TxA2 was found to be 105 more stable than TxA2, and surprisingly was only slightly less stable than F2-TxA2. Preliminary biol. studies showed that F-TxA2 has similar potency as TxA2 toward inducing platelet aggregation but was superior to F2-TxA2 in activating integrin αIIbβ3. The synthesis is described of 10-F-thromboxane A2 I, a stable mimic of TxA2 (105 x more stable) with similar potency as TxA2 toward inducing platelet aggregation. In the experiment, the researchers used 2,5-Dimethoxytetrahydrofuran(cas: 696-59-3Reference of 2,5-Dimethoxytetrahydrofuran)
2,5-Dimethoxytetrahydrofuran(cas: 696-59-3) is a member of ether. When aromatic ethers are exposed to halogen in the presence or absence of a catalyst, they undergo halogenation, such as bromination.Reference of 2,5-Dimethoxytetrahydrofuran
Referemce:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem