Category: 942603-91-0

Masschelein, Kurt G. R. published the artcileExploiting the regioselectivity of pyroglutamate alkylations for the synthesis of 6-azabicyclo[3.2.1]octanes and 4-azabicyclo[3.3.0]octanes, HPLC of Formula: 942603-91-0, the publication is Tetrahedron (2007), 63(22), 4712-4724, database is CAplus.

The preparation of 6-azabicyclo[3.2.1]octanes and 4-azabicyclo[3.3.0]octanes via regioselective alkylation and ring closure of pyroglutamates is described. Depending on the N-protecting group of pyroglutamates, the reactivity can be directed to the formation of 6-azabicyclo[3.2.1]octanes, e.g. I, or 4-azabicyclo[3.3.0]octanes, e,.g. II, which are conformationally restricted glutamate analogs. The stereoselectivity is also discussed.

Tetrahedron published new progress about 942603-91-0. 942603-91-0 belongs to esters-buliding-blocks, auxiliary class Other Aliphatic Fused-Heterocycles, name is Ethyl 2-methylene-5-oxohexahydro-1H-pyrrolizine-7a-carboxylate, and the molecular formula is C11H15NO3, HPLC of Formula: 942603-91-0.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Roecker, Anthony J. published the artcileDiscovery of selective, orally bioavailable, N-linked arylsulfonamide Na_v1.7 inhibitors with pain efficacy in mice, Synthetic Route of 942603-91-0, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(10), 2087-2093, database is CAplus and MEDLINE.

The voltage-gated sodium channel Na_v1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a variety of painful disorders and loss-of-function mutations affording insensitivity to pain. Unfortunately, drugs thought to garner efficacy via Na_v1 inhibition have undesirable side effect profiles due to their lack of selectivity over channel isoforms. Herein we report the discovery of a novel series of orally bioavailable arylsulfonamide Na_v1.7 inhibitors with high levels of selectivity over Na_v1.5, the Na_v isoform responsible for cardiovascular side effects, through judicious use of parallel medicinal chem. and physicochem. property optimization. This effort produced inhibitors such as compound 5 with excellent potency, selectivity, behavioral efficacy in a rodent pain model, and efficacy in a mouse itch model suggestive of target modulation.

Bioorganic & Medicinal Chemistry Letters published new progress about 942603-91-0. 942603-91-0 belongs to esters-buliding-blocks, auxiliary class Other Aliphatic Fused-Heterocycles, name is Ethyl 2-methylene-5-oxohexahydro-1H-pyrrolizine-7a-carboxylate, and the molecular formula is C11H15NO3, Synthetic Route of 942603-91-0.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics