Detail of "317357-42-9"

CAS Number:
317357-42-9
Name:
1,2-Pyrrolidinedicarboxylicacid, 4-(2-naphthalenyloxy)-, 1-(1,1-dimethylethyl) ester, (2S,4S)-
Molecular Structure:
Formula:
C20H23 N O5
Molecular Weight:
357.4
Synonyms:
(2S,4S)-BOC-4-(2-NAPHTHYLOXY)-PYRROLIDINE-2-CARBOXYLIC ACID;(2S,4S)-1-(TERT-BUTOXYCARBONYL)-4-(2-NAPHTHYLOXY)-2-PYRROLIDINECARBOXYLIC ACID
Hazard Symbols:
Safety:
Hazard Codes Xi
Details

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(2S,4S)-Boc-4-(2-naphthyloxy)-Pro-OH

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(2S,4S)-1-(TERT-BUTOXYCARBONYL)-4-(2-NAPHTHYLOXY)-2-PYRROLIDINECARBOXYLIC ACID

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4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist: All Rights Reserved. 4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist. Chiba, Jun; Iimura, Shin; Yoneda, Yoshiyuki; Sugimoto, Yuichi; Horiuchi, Takao; Muro, Fumito; Ochiai, Yuichi; Ogasawara, Tomomi; Tsubokawa, Masao; Iigou, Yutaka; Takayama, Gensuke; Taira, Tomoe; Takata, Yoshimi; Yokoyama, Mika; Takashi, Tohru; Nakayama, Atsushi; Machinaga, Nobuo (Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical, Co., Ltd. 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan).Some commonly used reagents like 317357-42-9 is used in this experiment. Chemical & Pharmaceutical Bulletin, 54(11), 1515-1529 (English) 2006 Pharmaceutical Society of Japan. CODEN: CPBTAL. ISSN: 0009-2363. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27 A novel series of benzoic acid derivs. as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC50 = 1.6 nM each) and moderate lipophilicity (Log D = 2.0, 1.8). Furthermore, 15e (I) demonstrated efficacy in murine asthma model at an oral dose of 30 mg/kg. .