The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride(SMILESS: Cl.F[C@@H]1CCNC1,cas:136725-55-8) is researched.HPLC of Formula: 21778-81-4. The article 《Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:136725-55-8).
We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative MT-3014 (1, I). A previous compound introduced was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the core stilbene structure. We discovered pyrazolo [1,5-a] pyrimidine as a new lead scaffold by structure-based drug design utilizing a co-crystal structure with PDE10A. The lead compound was optimized for in vitro activity, solubility, and selectivity against human ether-a-́go-go related gene cardiac channel binding. We observed that I shows excellent efficacy in rat conditioned avoidance response test and suitable pharmacokinetic properties in rats, especially high brain penetration.
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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem