- SYNTHESIS AND STRUCTURE OF , A PLATINUM(II) COMPLEX CONTAINING THE NEW LIGAND (DI-t-BUTYL)CYCLOBUTYLMETHYLPHOSPHINE
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The synthesis and spectral properties of trans-dichlorobis((di-t-butyl)cyclobutylmethylphosphine)platinum(II), , and of the new phosphine (di-t-butyl)cyclobutylmethylphosphine, , are described.The crystal structure of the Pt complex has been determined.The material crystallizes in the monoclinic system, space group C52h-P21/c, with two formula units in a cell of dimensions a 8.521(2), b 12.774(1), c 14.374(2) Angstroem, β 104.71(2) deg.A total of 5667 unique reflections were measured on a CAD4 diffractometer at 113 K.The final value of R(F) is 0.028 for those 4223 reflections having Fo2 > 3?(F2).The crystal structure consists of the packing of discrete neutral molecules of .A crystallographic center of symmetry is imposed on each molecule.Important intramolecular distances include Pt-P, 2.353(1) and Pt-Cl, 2.306(1) Angstroem.The shortest non-bonding distance between the Cl atom and a carbon atom of a t-Bu group is Cl...C(4), 3.387(3) Angstroem.No interaction between the Pt atom and the cyclobutane ring is observed.The absence of extreme steric congestion in the complex may explain the lack of such an interaction.
- Simms, Barbara L.,Ibers, James A.
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- Rearrangement of the Grignard reagent from 1-methylcyclobutylmethyl bromide: origins of the methyl substituent effect
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1-Methyl substitution leads to a small decrease (ca. 0.45) in the rate of the ring cleavage rearrangement of cyclobutylmethylmagnesium bromide.Comparison with literature data for 3- and 5-membered rings indicates that the methyl substituent shifts the equilibrium in the direction of ring cleavage, mostly by stabilization of the double bond of the open isomer, and possibly partly by destabilization of the organometallic function of the cyclic isomer.The reaction rate is decreased in both directions, probably because of increased transition state steric repulsions.
- Hill, E. Alexander,Hallade, Marc W.
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- Synthesis method of analgesic intermediate bromomethyl cyclobutane
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The invention relates to a synthesis method of analgesic intermediate bromomethyl cyclobutane. The synthesis method comprises the following steps: by taking ethylene and acrylic acid as starting materials, carrying out Diels-Alder reaction to obtain cyclobutanecarboxylic acid, then reducing to obtain cyclobutanemethanol, and then brominating to obtain high-purity bromomethyl cyclobutane, wherein the total yield reaches more than 65%. The synthesis method provided by the invention has the advantages of available raw materials, mild reaction conditions, simple postprocessing operation, small environmental pollution, short reaction time, high reaction operational safety, high reaction yield, good product quality and low cost, and industrial production is facilitated.
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Paragraph 0009; 0010; 0011; 0012; 0013; 0014
(2017/07/21)
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- METHOD FOR PRODUCING (BROMOMETHYL)CYCLOPROPANE AND (BROMOMETHYL)CYCLOBUTANE
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The present invention relates to a method for obtaining high purity (bromomethyl)cyclopropane and (bromomethyl)cyclobutane, starting respectively with cyclopropylmethanol and cyclobutylmethanol, under synthesis conditions that enable high productivity and high yield.
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Paragraph 0064; 0065
(2016/12/22)
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- 2-PHENYLPYRIDINE DERIVATIVE
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The present invention relates to a novel 2-phenylpyridine derivative or a salt thereof, wherein the pyridine ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.
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- Piperazine derivatives
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The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
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- Triazole derivatives
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The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
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- Indole derivatives as 5-HT1-like agonists
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Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is a substituted alkylene; C3 -C7 cycloalkyl optionally substituted with HO; C3 -C6 alkenyl optionally substituted with aryl; C5 -C7 cycloalkenyl; or C3 -C6 alkynyl; R2 is H; halo; F3 C; NC; R8 R9 NOC; a substituted alkylene; R8 R9 NO2 S; R10 S(O)m ; R12 CON(R11); R10 SO2 N(R11); R8 R9 NOCN(R11); R10 O2 CN(R11); R13 (CH2)n CH=CH; or R7 O are selective 5-HT1 -like receptor agonists useful in the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.
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- Syntheses with Aliphatic Dialdehydes, XXXVIII. - Synthesis and Properties of Cycloalkylmalonaldehydes
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Vilsmeier formylation of cycloalkyl-substituted enol ethers (7,14a - c,23) yields the cycloalkylmalonaldehydes 1 - 5 for the first time.In solution 1 - 5 exist in the (E)-s-(E) enol form as vinylogous carboxylic acids.The reaction of 1 - 5 with suitable electrophiles and nucleophiles leads to cycloalkyl-substituted open-chain (29,30), carbocyclic (31) as well as heterocyclic compounds (32-40) with peculiar properties due to the presence of the lipophilic cycloalkyl group.
- Reichardt, Christian,Ferwanah, Abdel-Rahman,Pressler, Wilfried,Yun, Kyeong-Yeol
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p. 649 - 679
(2007/10/02)
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- The Ring-opening Reactions of Cyclobutylmethyl and Cyclobutenylmethyl Radicals
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Rate constants for the ring-opening reactions of cyclobutylmethyl, 1-cyclobutyl-1-methylethyl, and cyclobut-2-enylmethyl radicals have been determined over a range of temperatures by kinetic e.p.r. spectroscopy.The results can be represented by equations (i) - (iii), respectively.The results are compared with those for ring log(k3/s-1) = (13.1 +/-1.4) - (49.8 +/-7.5 kJ mol-1)/2.3RT (i) log(k5/s-1) = (13.6 +/-1.6) - (58.1 +/-9.0 kJ mol1-)/2.3RT (ii) log (k10/s-1) = (12.2 +/-1.4) - (42.2 +/-8.0 kJ mol-1)/2.3RT (iii) opening of other cycloalkylmethyl radicals.The rate constants for self-reaction of n-pentyl radicals in toluene solution have also been measured over a temperature range and found to fit relation (iv). log(2kt/dm3 mol-1 s-1) = (12.3 +/-0.7) - (10.5 +/-3 kJ mol-1)/2.3RT (iv)
- Ingold, Keith U.,Maillard, Bernard,Walton, John C.
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p. 970 - 974
(2007/10/02)
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- N-alkyl-14-hydroxymorphinans and derivatives
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There is provided a novel and high yield procedure for transforming acid salts of 14-alkanoyloxymorphinans and derivatives thereof into the corresponding N-alkyl-14-hydroxymorphinans wherein the alkyl moiety on the nitrogen contains the same number of carbon atoms as that previously in the 14-alkanoyl moiety. In the process of the present invention, the acid is neutralized to the free base, the alkanoyl moiety at the 14-oxy then spontaneously shifts to the nitrogen and is subsequently reduced to the corresponding alkyl moiety. O-dealkylation at C-3, where an alkoxy group is originally present, is carried out in the usual manner. There is also provided a readily produced and readily disassociated adduct of the corresponding 14-hydroxy-N-alkanoyl morphinan-6-alkylene ketal with benzene, tetrahydrofuran, and the like.
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