1515-89-5Relevant academic research and scientific papers
Cobalt-Catalysed Reductive Etherification Using Phosphine Oxide Promoters under Hydroformylation Conditions
Beller, Matthias,Delolo, Fábio G.,Fessler, Johannes,Gusevskaya, Elena V.,Junge, Kathrin,Neumann, Helfried,dos Santos, Eduardo N.
supporting information, (2022/02/19)
A phosphine-oxide-promoted, cobalt-catalysed reductive etherification using syngas as a reductant is reported. This novel methodology was successfully used to prepare a broad range of unsymmetrical ethers from various aldehydes and alcohols containing diverse functional groups, and was scaled-up to multigram scale under comparably mild conditions. Mechanistic experiments support an acetalization–hydrogenation sequence.
PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY
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Paragraph 0356, (2016/10/07)
PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Paragraph 0411; 0412, (2013/05/08)
The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Page/Page column 188, (2011/11/01)
The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
New method for the synthesis of benzyl alkyl ethers mediated by FeSO 4
Joshi, Girdhar,Adimurthy, Subbarayappa
experimental part, p. 720 - 728 (2011/03/22)
The synthesis of benzyl alkyl ethers from benzyl bromides and alcohols using FeSO4 as a recoverable and reusable mediator has been described without use of base and cosolvent under mild conditions.
An improved synthesis of the selective EP4 receptor agonist ONO-4819
Ohta, Chisa,Kuwabe, Shin-Itsu,Shiraishi, Tai,Shinohara, Ikuo,Araki, Hiroshi,Sakuyama, Shigeru,Makihara, Takayuki,Kawanaka, Yasufumi,Ohuchida, Shuichi,Takuya, Seko
experimental part, p. 8298 - 8308 (2010/02/17)
(Chemical Equation Presented) An improved synthesis of the highly selective EP4-receptor agonist ONO-4819 has been developed. The previous synthesis suffered from several drawbacks, in which a critical one is the difficulty in the removal of byproducts leading to unsatisfactory quality of the active pharmaceutical ingredient (API). Furthermore, on stereoselective reduction of an enone intermediate by binaphthol-modified lithium aluminum hydride, low concentration of the reaction conditions and tedious purification procedures to remove excess binaphthol were critical issues for the manufacturing process of the API. In the improved process,we have developed improved conditions using γ-thiobutyrolactone as sulfur source instead of potassium thioacetate to introduce the sulfur-containing C4 side chain without formation of byproducts. For stereoselective synthesis of the chiral alcohol, (-)-DIP-chloride reduction is found to be the best method, which can improve not only the enantioselectivity but also the workload for removing the chiral modifier in a purification process. Furthermore, benzoyl and tert-butyldimethylsilyl groups as protecting groups for hydroxyl functions were used for precise process controls of all intermediates. By changing these protecting groups, the purity of ONO-4819 was strictly controlled through crystalline intermediates. Thus, an improved robust process for ONO-4819 with a high chemical purity was developed. 2009 American Chemical Society.
2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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Page/Page column 38-39, (2010/02/08)
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
5-thia-ω-substituted phenyl-prostaglandin E derivatives, process for producing the same and drugs containing the same as the active ingredient
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, (2008/06/13)
The present invention relates to 5-thia-ω-substituted phenylprostaglandin E derivatives of the formula (I) (wherein, all the symbols are as defined in the specification), process for producing them and pharmaceutical compositions comprising them as active
γ(v)-SUBSTITUTED PHENYL-PROSTAGLANDIN E DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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, (2008/06/13)
An ω-substituted phenyl-prostaglandin derivative of formula (I), a process for the preparation thereof, a medicament comprising it as active ingredient (all symbols have the same meaning as described in the specification). The compounds of the formula (I)
3,7-dithiaprostanoic acid derivative
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, (2008/06/13)
A 3,7-dithiaprostanoic acid derivative of the formula (I) STR1 (wherein, R1 is OH, C16 alkyloxy, NR6 R7 (R6, R7 are H, C16 alkyl.); R2 is H, OH; R3 is single bond, C16 alkylene; R4 is (i) C18 alkyl substituted by C16 alkyloxy, halogen etc., (ii) phenyloxy
