Reference

Antifungal 2-substituted phthalimidines

Antifungal 2-substituted phthalimidines. Schwan, Thomas J. (Morton-Norwich Products, Inc. 939-26-4 and 102-47-6 are also occured in this study., USA). U.S. US 3993617 23 Nov 1976, 2 pp. (English). (United States of America). CODEN: USXXAM. CLASS: IC: C07D209-46. NCL: 260325000PH. APPLICATION: US 75-627229 30 Oct 1975. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 5 Phthalimidine with NaH, then 3,4-Cl2C6H3CH2Cl or 2-(bromomethyl)naphthalene gave I (R = 3,4-Cl2C6H3, 2-naphthyl), useful as fungicides. .

SAR of 2-benzyl-4-aminopiperidines NK1 antagonists

Part 2. Synthesis of CGP 49823. Veenstra, Siem J.; Hauser, Kathleen; Schilling, Walter; Betschart, Claudia; Ofner, Silvio (Research Department, CIBA-GEIGY AG, Basel CH-4002, Switz.). Bioorganic & Medicinal Chemistry Letters, 6(24), 3029-3034 (English) 1996 Elsevier. CODEN: BMCLE8. ISSN: 0960-894X. DOCUMENT TYPE: Journal CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1 CGP 49823 is a potent NK1 antagonist which is centrally active after oral administration. 186826-45-9 and 102-47-6 are also in the experiment. The SAR of the C-2 substituent was investigated with respect to the affinity to the NK1 receptor. A practical synthesis of CGP 49823, suitable for scale-up, was developed. The key-step, a tandem acyliminium ion cyclization/Ritter reaction, gave trans 2-benzyl-4-acetamidopiperidines with high diastereoselectivity. .