- Sulfur ylides 9. Resonance electron capture by molecules of keto-stabilized sulfur ylides containing a phthalimide fragment
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The mass spectra of negative ions of keto-stabilized sulfur and phosphorus ylides (obtained from amino acids) and products of their thermal conversion are studied. The most characteristic peaks in the mass spectra of ylides belong to negative molecular ions and to [M - H]- ions. Peaks of fragment ions in the mass spectra of ylides and products of their thermal conversion coincide both in mass numbers and resonance energies.
- Mavrodiev,Furlei,Lakeev,Galin,Tolstikov
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Read Online
- Preparation method of ftibamzone
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The invention discloses a preparation method of ftibamzone. The preparation method comprises the following steps: firstly, preparing 3-phthalimide butanone from phthalimide potassium salt and 3-chlorobutanone; reacting the 3-phthalimide butanone with dry hydrogen bromide gas in a dimethyl sulfoxide solution to prepare a dimethyl sulfoxide solution of 3-phthalimide-2-oxy-n-butyraldehyde; dropwise adding a thiosemicarbazide solution into the dimethyl sulfoxide solution of the 3-phthalimide-2-oxy-n-butyraldehyde, controlling the reaction temperature, carrying out heat preservation reaction to prepare a crude product, and recrystallizing the crude product to obtain the ftibamzone. The technical scheme has the advantages of few reaction steps, high yield and high purity.
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Paragraph 0017-0018
(2021/02/10)
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- Preparation method of 3-phthalimide-2-oxy-n-butyraldehyde thiosemicarbazide
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The invention relates to a preparation method of 3-phthalimide-2-oxy-n-butyraldehyde thiosemicarbazide (I). The preparation method comprises the steps: adopting alanine and N-ethoxycarbonyl phthalimide as a starting material, and performing aminoacylation, methyl-lithium addition, an oxidation reaction and a condensation reaction so as to obtain the target product 3-phthalimide-2-oxy-n-butyraldehyde thiosemicarbazide (I). The method for synthesizing 3-phthalimide-2-oxy-n-butyraldehyde thiosemicarbazide has the advantages of few reaction steps, simple operation, suitability for large-scale production and the like.
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- Method for synthesizing 3 - phthalatic imide - 2 - oxo-butyl - 1, 2 - double-thiosemicarbazone method
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The invention relates to a novel method of synthesizing 3-phthalimide-2-oxobutryaldehyde-1, 2-bis-thiosemicarbazide. The novel method comprises the following steps: synthesizing 3-nitro-2-butanol with acetaldehyde and nitroethane as starting raw materials, then carrying out reduction on 3-nitro-2-butanol to generate 3-amino-2-butanol, carrying out reaction on 3-amino-2-butanol and phthalic anhydride to generate N-(1-methyl-2-hydroxypropyl) phthalimide, respectively carrying out oxidation by two steps to form 3-phthalimide-2-oxo-butyraldehyde, and finally carrying out condensation on 3-phthalimide-2-oxo-butyraldehyde and thiosemicarbazide to obtain a target product. The 3-phthalimide-2-oxobutryaldehyde-1, 2-bis-thiosemicarbazide has obvious inhibition action on replication of herpes simplex I type (HSV-I) and II I type (HSV-II) viruses in tissue culture cells; at present, the 3-phthalimide-2-oxobutryaldehyde-1, 2-bis-thiosemicarbazide is mainly clinically used for treating skin diseases caused by herpesvirus and sexually transmitted diseases caused by human papillomavirus (HSV) and has good curative effect.
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Paragraph 0065; 0066; 0087; 0088
(2017/04/12)
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- Aldehyde-selective wacker-type oxidation of unbiased alkenes enabled by a nitrite co-catalyst
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Breaking the rules: Reversal of the high Markovnikov selectivity of Wacker-type oxidations was accomplished using a nitrite co-catalyst. Unbiased aliphatic alkenes can be oxidized with high yield and aldehyde selectivity, and several functional groups are tolerated. 18O-labeling experiments indicate that the aldehydic O atom is derived from the nitrite salt. Copyright
- Wickens, Zachary K.,Morandi, Bill,Grubbs, Robert H.
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supporting information
p. 11257 - 11260
(2013/11/06)
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- Efficient preparation of biologically important 1,2-amino alcohols
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An efficient three-step methodology developed for the preparation of 1,2-amino alcohols. In the first step a rapid coupling between bromoketones and potassium phthalimide in ionic liquid produced-phthalimido ketones in quantitative yields, which is followed by a facile reduction using NaCNBH 3 in acetic acid to give corresponding phthalimido alcohols and finally effecting hydrazinolysis in water at 60C to yield biologically important 1,2-amino alcohols.
- Gupta, Pankaj,Rouf, Abdul,Shah, Bhahwal A.,Mukherjee, Debaraj,Taneja, Subhash C.
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p. 505 - 519
(2013/01/15)
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- Synthesis and antiviral activity of phthiobuzone analogues
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A series of phthiobuzone analogs, prepared from potassium phthalimide or phthalandione, have been evaluated for their antiviral activities. Among the candidates, compounds 5j and 5k, which contain the substituted 4-halogenated phenyl ring at N-4′,4″ position, show more potent antiviral activity than phthiobuzone against herpes simplex virus 1 (IC50=8.56 and 2.85 μ/ml, respectively) and herpes simplex virus 2 (IC50=1.75 and 4.11μg/ ml, respectively). Compounds 9c and 9d with a propylene linker between the phthalimide and bisthiosemicarbazone moieties display similar antiviral potency against herpes simplex virus 1 (IC50=2.85 and 4.11 μg/ml, respectively).
- Yang, Ya-Jun,Zhao, Jing-Hua,Pan, Xian-Dao,Zhang, Pei-Cheng
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experimental part
p. 208 - 211
(2010/08/06)
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- Synthesis and cytotoxic activity of heterocycle-substituted phthalimide derivatives
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A series of heterocycle-substituted phthalimide derivatives were synthesized. Structurally diverse derivatives with heterocyclic rings, including furan, imidazo[1,2-a]pyridine, 1,3,4-thiadiazine, imidazo[2,1-b][1,3,4] thiadiazine, pyrazole, 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine, thiazole and thiazoline, were obtained by the reactions of α-bromoketone intermediate with various nucleophiles containing oxygen, nitrogen and sulfur atom. Their cytotoxic activity was also evaluated against five human cancer cell lines in vitro.
- Yang, Ya Jun,Yang, Ya Nan,Jiang, Jian Shuang,Feng, Zi Ming,Liu, Hong Yan,Pan, Xian Dao,Zhang, Pei Cheng
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scheme or table
p. 902 - 904
(2011/11/30)
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- Concise synthesis of 1H-pyrazin-2-ones and 2-aminopyrazines
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Convenient syntheses of 1H-pyrazin-2-ones and 2-aminopyrazines are described. By coupling Boc-protected amino acids with α-amino ketones or with amino alcohols and subsequent oxidation, 1H-pyrazin-2-ones were obtained. Transformation into the corresponding pyrazine triflates and substitution with primary or secondary amines led to 2-aminopyrazines. Since these syntheses take advantage of the use of readily available starting materials (e.g., amino acids, aminoalcohols and amines) a variety of the entitled structures can be obtained in few, high yielding steps.
- Adam, Isabelle,Orain, David,Meier, Peter
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p. 2031 - 2033
(2007/10/03)
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- AMIDOACETONE ENOLATE ANIONS: ALKYLATION AND MICHAEL REACTION
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The lithyum enolate derived from benzamidoacetone (1) can be regiospecifically alkylated at C(1) and stereospecifically added in conjugate fashion to cyclohexenone without resorting to protection of free NH.Comparison is made with alkylations of methyl hippurate.
- Hoye, Thomas R.,Duff, Steven R.,King, Rita S.
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p. 3433 - 3436
(2007/10/02)
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