- Synthesis method of 5-fluoro-2-(1-bromocyclopropyl) pyridine
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The invention relates to a synthesis method of 5-fluoro-2-(1-bromocyclopropyl) pyridine. 1,4-butyrolactone, ethyl 4-bromobutyrate and 5-fluoro-2-mercaptopyridine are used as raw materials to prepare 5-fluoro-2-(1-bromocyclopropyl) pyridine through eleven steps of reaction. A synthetic route of the 5-fluoro-2-(1-bromocyclopropyl) pyridine is as follows: (as described in the specification). The invention has the advantages that the synthesis method of 5-fluoro-2-(1-bromocyclopropyl) pyridine improves the yield and provides an efficient synthesis method for the synthesis of the compound.
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Paragraph 0005; 0016; 0027; 0038
(2019/08/01)
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- PRODUCTION METHOD OF HETEROCYCLIC MERCAPTO COMPOUND
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A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of -O-, -S-, -NH-, and -NR1-; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or -NR2-; R2represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.
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Page/Page column 45
(2008/06/13)
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- HAIR PROCESSING AGENT AND METHOD FOR PERMANENT WAVING HAIR
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Provided are hair processing agents capable of permanent waving hair even at a neutral to weakly acidic pH range that causes less irritation to the skin, and hair processing agents in which an unpleasant odor is masked. Hair processing agents contain at least one compound represented by the formula (2). Hair processing agents contain a compound of the formula (2) and at least one compound (ii) selected from thioglycolic acid, thiolactic acid, cysteine, acetylcysteine, cysteamine, acylcysteamine, salts thereof and ester derivatives thereof. Hair processing agents contain a compound of the formula (2), a surfactant and water, and are emulsified. Hair processing agents contain a compound of the formula (2) and a specific perfume. wherein X is a structure selected from -O-, -S-, -NH- and -NR1-; R1 is an alkyl group of 1 to 6 carbon atoms; Y is an oxygen atom or a sulfur atom; in the formula (1), Z is a divalent organic residue having at least one mercapto group; in the formula (2), R is a divalent organic residue optionally having a mercapto group; and R2 is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms.
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Page/Page column 115-116
(2008/06/13)
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- Complexes of cyclic polyaza chelators with cations of alkaline earth metals for enhanced biological activity
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Cyclic polyaza chelators that possess high affinity and specificity for first transition series metal cations exhibit an unanticipated improvement in biological activity when administered as complexes with cations of the alkaline earth metals, Ca(II) and Mg(II), most notably Ca(II). By virtue of this improvement, these complexes are particularly effective in the treatment of pathological conditions, including ischemia and ischemia-reperfusion injury.
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Page/Page column 12
(2010/02/11)
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- Chemoenzymatic enantioselective synthesis of 3-hydroxy-2-pyrrolidinones and 3-hydroxy-2-piperidinones
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The enantioselective synthesis of 3-hydroxypyrrolidin-2-ones and 3-hydroxy piperidin-2-ones has been carried out in high enantiomeric excess employing immobilized lipase from Pseudomonas cepacia.
- Kamal, Ahmed,Ramana, K. Venkata,Ramana, A. Venkata,Babu, A. Hari
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p. 2587 - 2594
(2007/10/03)
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- Heterocyclic nonionic X-ray contrast agents V: A facile conversion of 2-tetrahydrofuroamides into α-hydroxy-δ-valerolactams and a general synthesis of lactams conjugated to 2,4,6-triiodoisophthalamides
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The synthesis of 2,4,6-triiodoisophthalamides substituted by a lactam moiety is described. A tandem ring opening-ring closure methodology consisting of a regiospecific ether cleavage of the tetrahydrofuroanilide 14b, followed by lactamization to α-oxygenated anilides 15b or 16b, gave α-O-functionalized-δ-valerolactams 12b or 13b, respectively. This approach is also compatible with the presence of ester and carbonyl chloride functions on the triiodophenyl moiety. A general synthesis of lactams 34-39 was also achieved. Further chemical modifications led to water soluble unsubstituted-lactams (34d, 35d, 37d) and α-hydroxyl-lactams [42(d,e), 13(d,e) and 43d] that are of interest as X-ray contrast agents.
- Marinelli,Arunachalam,Diamantidis,Emswiler,Fan,Neubeck,Pillai,Wagler,Chen,Natalie,Soundararajan,Ranganathan
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p. 11177 - 11214
(2007/10/03)
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- Nonionic X-ray contrast agents, compositions and methods
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Triiodinated isophthalamide derivatives, useful as X-ray contrast agents, having at least one amide group derived from the amino-alcohol, 3-(N-2-hydroxyethyl)amino-1,2-propanediol, which provides high water solubility and low mammalian toxicity, and methods of preparing them. Methods of preparing 3-(N-2-hydroxyethyl)amino-1,2-propanediol are provided.
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- Trispirododecane-4,8,12-trione and Other Oligomers of Carbonylcyclopropane. The Organozinc Route
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1-Bromocyclopropanecarboxylic acid (8) and its chloride (9) were prepared from γ-butyrolactone on a 20-100-g scale.Dehalogenation of 9 with zinc-copper couple in acetonitrile gave not only the known dispiro octane-4,8-dione (3) but also the aesthetically pleasing title compound 10 and 6-cyclopropylidene-5-oxaspirohexan-4-one (11) as well as tetracyclic α-alkylidene-γ-butyrolactone 12, i.e., 3-(oxodispirooctan-4-ylidene)tetrahydro-2-furanone. "Zinc carbon enolate" 13a is considered to be an important intermediate en route to 10 in solventacetonitrile.The X-ray crystal structure of 10 shows the molecule to be nearly planar with very short distal cyclopropane carbon-carbon bonds .
- Hoffmann, H. Martin R.,Eggert, Ulrike,Walenta, Angela,Weineck, Edeltraut,Schomburg, Dietmar,et al.
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p. 6096 - 6100
(2007/10/02)
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- Process for preparing (+)-2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid and related compounds
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2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds of the formula, STR1 in which Y is OH; O- M+, wherein M is an alkali metal; or NRR', wherein R is lower alkyl and R' is lower alkyl or aryl, or NRR' is the residue of a saturated cyclic amine, are prepared from pyrrole.
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- Lactones, I: Synthesis of Dihydroxylated Diphenylethanamines via &α-Amino-&γ-lactones
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Treatment of α-amino-γ-lactones with phenyllithium yields the 2-amino-1,1-diphenylalkane-1,4-diols 2a-f which can be classified as dihydroxylated diphenylethanamines.
- Lehmann, Jochen
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p. 241 - 249
(2007/10/02)
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