- 2 - Morpholine alkone salt and its preparation method, 2 - process for preparation of method (by machine translation)
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The invention relates to a 2 - morpholine alkone salt and its preparation method, 2 - process for preparation of method, which belongs to the technical field of the synthesis of pharmaceutical intermediates. The 2 - morpholine alkone salt preparation method, comprises the following steps: the amino protecting group with N - (2 - hydroxyethyl) glycine, catalyst in the reflux solvent heating reflux reaction, with amino protecting group prepared 2 - morpholone; said catalyst is paratoluene sulfonic acid or concentrated sulfuric acid; the amino protecting group with 2 - morpholone acidification is carried out by removing the protecting group 2 - morpholine alkone salt. 2 - Morpholone is 2 - morpholine alkone salt in the solvent in the reaction with the alkali. The invention of 2 - morpholine alkone salt and 2 - morpholone in the preparation method, the use of cheap raw material, short synthetic route, all reaction intermediate and final products do not need column chromatographic purification. The method of low cost, high efficiency, and high product purity. (by machine translation)
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Paragraph 0095; 0103; 0112; 0122; 0131; 0140
(2018/10/24)
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- Optimization of gefitinib analogues with potent anticancer activity
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The interactions of gefitinib (Iressa) in EGFR are hydrogen bonding and van der Waals forces through quinazoline and aniline rings. However the morpholino group of gefitinib is poorly ordered due to its weak electron density. A series of novel piperazino analogues of gefitinib where morpholino group substituted with various piperazino groups were designed and synthesized. Most of them indicated significant anti-cancer activities against human cancer cell lines. In particular, compounds 52-54 showed excellent potency against cancer cells. Convergent synthetic approach has been developed for the synthesis of gefitinib intermediate which can lead to gefitinib as well as numerous analogues.
- Yin, Kai-Hao,Hsieh, Yi-Han,Sulake, Rohidas S.,Wang, Su-Pei,Chao, Jui-I.,Chen, Chinpiao
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supporting information
p. 5247 - 5250
(2015/01/08)
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- Triazolium Carbene Catalysts and Stereoselective Bond Forming Reactions Thereof
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Provided herein are triazolium carbine catalysts useful for asymmetric hydration, fluorination, and deuteration, and processes for their preparation. Also provided are synthetic reactions in which these catalysts are used, in particular, in stereoselective formation of carbon-chlorine, carbon-hydrogen, carbon-fluorine, and carbon-deuterium bonds.
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Page/Page column 6-7
(2011/10/04)
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- Carbocyclic side chain containing metalloprotease inhibitors
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The compounds have a structure according to the following Formula (I): are effective in treating conditions characterized by excess activity of these enzymes.
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- Piperizinones as modulators of chemokine receptor activity
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The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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- MORPHOLINONE AND MORPHOLINE DERIVATIVES AND USES THEREOF
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This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human α 1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the α 1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
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- Morpholinones as light stabilizers
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The invention relates to new compounds containing 1-8 active groups of the type 3,3,6,6-polysubstituted 2-morpholinone and having the formula F(A'-Z)m-X(F),wherein m is a number from 1 to 8; X is an organic anchor group of valency m and in case that m is not 1, X may also be a direct bond, SO2, P or PO; A' is a monovalent group of the formula E containing one linking group; Z is a direct bond, -O-, -S-, -SO-, -SO2- or -NR'14-; provided that Z is -O-, -S-, -SO-, -SO2- or -NR'14- if m is 1 and the linking group in formula E is G3 or G5; G1 is hydrogen; C1-C18alkyl; C2-C18alkyl substituted by OH and/or phenyl; oxyl; OH; C2-C12cyanoalkyl; C2-C12cyanoalkoxy; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C3-C8alkenyloxy; C7-C12phenylalkyl; C7-C12phenylalkyl substituted by hydroxy, C1-C4alkyl and/or C1-C4alkoxy; C7-C15phenylalkoxy; C7-C15phenylalkoxy, which is substituted by C1-C4alkyl and/or C1-C4alkoxy; or G1 is C1-C8alkanoyl; C3-C5alkenoyl; C1-C18alkanoyloxy; C3-C8epoxyalkyl; or G1 is the linking group -R10-; G2 and G4 are, independently of one another, C1-C18alkyl, C5-C12cycloalkenyl, C5-C12cycloalkyl, or an oligocyclic hydrocarbon residue of 6-12 carbon atoms; G3 is as defined for G2 or is C1-C8hydroxyalkyl; or G2 and G3 together are (CH2)e, where e is a number from 4 to 11; or G5 is the linking group -R5-; G5 is as defined for G4 or is C1-C8hydroxyalkyl; or G4 and G5 together are (CH2)e, where e is number from 4 to 11; or G5 is the linking group -R5-; G6 is as defined for G4 or is hydrogen; or G6 is the linking group, which is a direct bond or -R5-; and other residues are as defined in claim 1. The new compounds are effective as stabilizers for organic material, especially coatings, against harmful effects of light, oxygen and/or heat.
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- Morpholine derivatives, compositions and medicinal use
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Compounds of formula (I): STR1 or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group, R1 is hydrogen or methyl, R2 is carboxyl or a group O--Z--CO2 H or an ester or amide thereof; a group O--E--NR3 R4 or a group O--E--OR5, wherein R3, R4 and R5 each represents hydrogen or C1-6 alkyl, Z is a C1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R2 ; a process for the production of such compounds and their use in treating hyperglycaemia and/or obesity.
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