- Aldehyde as a Traceless Directing Group for Regioselective C-H Alkylation Catalyzed by Rhodium(III) in Air
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The aromatic aldehyde as a traceless directing group for the regionselective C-H alkylation catalyzed by rhodium(III) under aerobic atmospheric conditions has been developed. The process involves an aldehyde assisted direct addition of C-H bond to unsaturated electrophiles of acrylates or acrylic acids, and the subsequent decarbonylation. A trace amount of water is found to favor the reaction.
- Chen, Si-Qi,Fan, Juan,Li, Chao-Jun,Li, Xin-Ran,Liu, Zhong-Wen,Shi, Xian-Ying
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supporting information
p. 1259 - 1264
(2020/03/13)
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- 1,4,5,6, 7,8-HEXAHYDRO-I^1S-TRIAZA-AZULENE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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The invention relates to 1,4,5,6,7,8-hexahydro-1,2,5-triaza-azulene derivatives of formula (II), wherein the chirality is as depicted below, (II) and their use as orexin receptor antagonists.
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Page/Page column 22
(2008/06/13)
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- 5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES
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The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
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Page/Page column 39
(2008/12/06)
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- LIGANDS AND CATALYSTS FOR PRODUCING ELASTOMERIC PROPYLENE POLYMERS
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A ligand useful to form a metallocene olefin polymerization catalyst comprises:wherein at least R3 and R4 are substituents having at least a bulk of a t-butyl group and, optionally, wherein R1 or R2 may be a bulky substituent group.
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- N-Arylalkylphenylacetamide derivatives
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N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities. STR1
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- N-arylalkylphenylacetamide derivatives
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N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities.
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- Aromatic Spiranes XX [1]: Syntheses of Dimethylsubstituted 2-Carboxymethyl-indan-1-ones and Benzylchlorides as Synthones for Syntheses of di- to tetramethylsubstituted Spirobiindandiones
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The isomeric dimethyl methylbenzoates 5, obtained from the bromides via Grignard reactions with dimethylcarbonate, were reduced with LiAlH4 to the hydroxymethyl derivatives 6. The latter were then transformed both to the benzylchlorides 7 (with SOCl2) and to the aldehydes 8 (with pyridinium chlorochromate). Knoevenagel-Doebner reaction of 8 afforded the acrylic acids 9 which (after hydrogenation to 11) were cyclized to the desired indanones 12 with polyphosphoric acid. On the other hand, 12c and 12e were prepared from dimethyl 3-chloropropiophenone (14) by warming with sulfuric acid. After NaH-catalyzed reaction with dimethylcarbonate, the indanones 12 gave the ketoesters 15 which then could be hydrogenated to the indanes 16. All reactions proceeded with satisfactory to excellent yields (60-90%).
- Neudeck
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p. 185 - 200
(2007/10/03)
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- Phenylacetamide derivatives and pharmaceutical compositions thereof
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The present invention provides novel phenylacetamide derivatives having the following formula STR1 wherein: X is a hydrogen, halogen, hydroxy, nitro, amino, R1, NR1 R2, NHR1 or OR1 wherein R1/su
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- Novel phenylacetamide derivatives and processes for the preparation thereof
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The present invention provides novel phenylacetamide derivatives having the following formula wherein:, X is a hydrogen, halogen, hydroxy, nitro, amino, R1, NR1R2, NHR1 or OR1 wherein R1 and R2 are an optionally substituted C1 8 alky
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