- Purines. LIX. An alternative synthesis of 7-alkyl-1-methyladenines by regioselective alkylation, fission, and reclosure of the adenine ring
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7-Alkyl-1-methyladenines (12a,b) have been synthesized from 1-alkyl-4- aminoimidazole-5-carboxamides (5a,b) in two steps [hence from adenine (1) in six steps]. The synthesis started with dehydration (using POCl3-HCONMe2) of 5a,b, rea
- Fujii,Saito,Suzuki,Kunugi
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- OXADIAZOLE TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS
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The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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- OXADIAZOLONES AS TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS
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The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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Paragraph 0169; 0170; 0173; 0174
(2018/06/12)
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- NEW TRPA1 ANTAGONISTS
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The present invention relates to bicyclic heterocyclic derivatives of Forrmula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.
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Page/Page column 35; 39
(2017/05/02)
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- Regioselective and efficient synthesis of N 7-substituted adenines, guanines, and 6-mercaptopurines
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A simple and efficient protocol for the preparation of N 7-substituted adenines, guanines, and 6-mercaptopurines is described. The key step is the regioselective preparation of 7-substituted 6-chloropurines which are building blocks for the div
- Maryska, Michal,Chudikova, Nadezda,Kotek, Vladislav,Dvorak, Dalimil,Tobrman, Tomas
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p. 501 - 507
(2013/07/26)
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- Purines. LXXV. Dimroth rearrangement, hydrolytic deamination, and pyrimidine-ring breakdown of 7-alkylated 1-alkoxyadenines: N(1)-C(2) versus N(1)-C(6) bond fission
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On treatment with boiling H2O for 5-6h, 1-alkoxy-7-alkyladenines (13) underwent hydrolytic cleavage of the N(1)-C(2) and the N(1)-C(6) bonds to produce the imidazole-5-carboxamidines (14) in 53-60% yields and the imidazole-5-carboxamides (18) i
- Itaya, Taisuke,Ito, Nobuaki,Kanai, Tae,Fujii, Tozo
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p. 832 - 841
(2007/10/03)
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- Deribosylation of Mesoionic Nucleosides in the Reaction with Lithium 2-Methylpropane-2-thiolate
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A series of mesoionic nucleosides related to 7-methylguanosine (I) was subjected to the action of a strong nucleophilic reagent, lithium 2-methylpropane-2-thiolate.Nucleophilic displacement of the β-D-ribofuranosyl portion appeared to be the main direction of the reaction.No dealkylation products were found in the reaction mixtures.
- Boryski, Jerzy,Golankiewicz, Bozenna
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p. 147 - 152
(2007/10/02)
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