HPLC of Formula: 202982-63-6On October 8, 1998 ,《Novel, Highly Potent Aldose Reductase Inhibitors: (R)-(-)-2-(4-Bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine- 4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (AS-3201) and Its Congeners》 was published in Journal of Medicinal Chemistry. The article was written by Negoro, Toshiyuki; Murata, Makoto; Ueda, Shozo; Fujitani, Buichi; Ono, Yoshiyuki; Kuromiya, Akemi; Komiya, Masanobu; Suzuki, Kenji; Matsumoto, Jun-ichi. The article contains the following contents:
A series of novel tetrahydropyrrolo[1,2-a]pyrazine derivatives were synthesized and evaluated as aldose reductase inhibitors on the basis of their abilities to inhibit porcine lens aldose reductase in vitro and to inhibit sorbitol accumulation in the sciatic nerve of streptozotocin-induced diabetic rats in vivo. Of these compounds, spirosuccinimide-fused tetrahydropyrrolo[1,2-a]pyrazine-1,3-dione derivatives showed significantly potent aldose reductase inhibitory activity. In the in vivo activity of these derivatives, 2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (I) (SX-3030) showed the best oral activity. The enantiomers of I were synthesized, and the biol. activities were evaluated. It was found that aldose reductase inhibitory activity resides in the (-)-I (AS-3201), which was 10 times more potent in inhibition of the aldose reductase (IC50 = 1.5 × 10-8 M) and 500 times more potent in the in vivo activity (ED50 = 0.18 mg/kg/day for 5 days) than the corresponding (+)-I (SX-3202). From these results, AS-3201 was selected as the candidate for clin. development. The absolute configuration of AS-3201 was also established to be (R)-form by single-crystal X-ray anal. In this article we report the preparation and structure-activity relationship of tetrahydropyrrolopyrazine derivatives including a novel aldose reductase inhibitor, AS-3201. In the part of experimental materials, we found many familiar compounds, such as (4-Chloro-2-fluorophenyl)methanamine hydrochloride(cas: 202982-63-6HPLC of Formula: 202982-63-6)
(4-Chloro-2-fluorophenyl)methanamine hydrochloride(cas: 202982-63-6) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).HPLC of Formula: 202982-63-6
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics