1559-02-0Relevant articles and documents
A convenient synthesis of cyclopropane malonyl peroxide
Terent'Ev, Alexander O.,Vil', Vera A.,Mulina, Olga M.,Pivnitsky, Kazimir K.,Nikishin, Gennady I.
, p. 345 - 345 (2014)
Cyclopropane-1,1-dicarbonyl peroxide was prepared in 85% yield by the reaction of diethyl cyclopropane-1,1-dicarboxylate with the urea hydrogen peroxide clathrate in the presence of methanesulfonic acid.
Polymers Containing Ring-Strain Energy. 1. New Monomers and Polymers Based on Cyclopropane, Norbornadiene, and Quadricyclane
Wright, Michael E.,Allred, Gary D.,Wardle, Robert B.,Cannizzo, Louis F.
, p. 4122 - 4126 (1993)
The synthesis and polymerization chemistry of 1,1-bis(XCH2)cyclopropane was studied.Treatment of 1 with base in the presence of α,ω-dihalides did not produce a polyether.However, treatment of 4 with the bis(alkoxide) derived from hexanediol afforded a polyether of low molecular weight n=3000, PD=3>.A general method for alkylating norbornadiene in the 2-position was developed.Treatment of norbornadiene with tert-BuOK, tetramethylethylenediamine (TMEDA), n-BuLi, and tributylchlorostannane (in that order) afforded 2-(tributylstannyl)norbornadiene in excellent yield.On the other hand, carbon electrophiles required the generation of the 2-(lithiocyanocuprate) in order to effect clean alkylation.Treatment of 2-norbornadiene (8a) with RMgX in the presence of (dppp)NiCl2 afforded the cross-coupling products 2-(XCH2)-norbornadiene in high yield.Polymerization of 9 in THF initiated by n-BuLi resulted in an elastomeric polymer (12) n=18,000, PD=1.5>.Photolysis of 12 in the presence of (Ph3P)2CuBr converted the pendant norbornadiene to quadricyclane (13).Heating of the photoisomerized sample to 180 deg C caused an exothermic (by DSC) reaction which corresponded to 59percent of theory (using the value 26 kcal/mol: quadricyclane -> norbornadiene).
Synthesis, crystal structure and bioactivity of N-(5-propyl-1,3,4- thiadiazol-2-yl)cyclopropanecarboxamide
Sun, Na-Bo,Jin, Jian-Zhong,Lei, Chao,He, Fang-Yue
, p. 7820 - 7822 (2013)
A new 1,3,4-thiadiazole compound with m.f. C9H 13N3OS, has been synthesized and confirmed by 1H NMR and HRMS. The single crystal structure of the 1,3,4-thiadiazole compound was determined by a single crystal X-ray diffraction study. The crystal belongs to the triclinic system, space group P-1 with a = 10.238(2), b = 10.325(2), c = 10.560(2) ?, α = 104.09(3), β = 109.50(3), γ = 93.40(3)°, Z = 4, V = 1008.4(3)?3, Mr = 211.28, Dc = 1.392 g/cm3, S = 0.98, μ = 0.29 mm-1, F(000) = 448, the final R1 = 0.0970 and wR2 = 0.2147 for 1776 were observed with I > 2Σ(I). X-ray indicated that two intermolecular hydrogen bonds N1-H1···N5, N4-H4···N2 were observed. The preliminary biological test shown that the synthesized compound has moderate herbicidal activity against Brassica campestris.
1, 1-cyclopropane dicarboxylic acid amide compound as well as preparation method and application thereof
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Paragraph 0024; 0028-0030, (2021/01/11)
The invention discloses a 1, 1-cyclopropane dicarboxylic acid amide compound as well as a preparation method and application thereof, and the structural formula of the 1, 1-cyclopropane dicarboxylic acid amide compound is as shown in a formula (I): in the formula (I), the structures of two substituted benzene rings are the same, the number of substituents R on each substituted benzene ring is 1-3,and the substituent R is selected from H, halogen, C1-C4 alkyl, C2-C4 ester group or C1-C3 alkoxy. The 1, 1-cyclopropane dicarboxylic acid amide compound provided by the invention is a novel compoundwith an efficient weeding effect, and provides a basis for research and development of novel herbicides.
Efficient cyclopropanation of aryl/heteroaryl acetates and acetonitriles with vinyl diphenyl sulfonium triflate
Zhou, Mingwei,Hu, Yimin,En, Ke,Tan, Xuefei,Shen, Hong C.,Qian, Xuhong
supporting information, p. 1443 - 1445 (2018/03/12)
A convenient method was developed for the cyclopropanation of aryl acetates and aryl acetonitrile using vinyl diphenyl sulfonium triflate salt. The newly developed conditions are simple, mild, and compatible with a wide range of functional groups, without the need to apply an inert atmosphere, or alkali bases.
A 4, 7 - diaza spiro [2.5] octane -7 - formic acid tert-butyl synthetic method
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Paragraph 0036; 0051; 0053; 0054, (2019/01/08)
The invention belongs to the technical field of chemical synthesis of N-heterocycle-containing drug intermediates, and particularly relates to a synthesis method of tert-butyl 4,7-diazaspiro[2.5]octyl-7-formate. By using diethyl malonate as a raw material, cyclization reaction, Hofmann reaction, hydrolysis reaction, acylation reaction for recyclization, reduction reaction and the like are performed to conveniently synthesize the target compound product. The method has the advantages of simple synthesis technique, cheap and accessible raw materials, mild reaction conditions, high controllability, low cost and high yield, and is convenient to operate.
Preparation method of compound
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Paragraph 0055; 0056; 0057; 0058; 0059, (2017/06/27)
The invention discloses a preparation method of a compound shown in the formula (I). The method is characterized by including the following steps of firstly, mixing the compound shown in the formula (I), a compound shown in the formula (III), strong alkali and weak acid salt and a catalyst to obtain a mixed solution; secondly, conducting heating and refluxing on the mixed solution obtained in the first step, and conducting post-processing to obtain the compound shown in the formula (I), wherein X is Cl, Br or I. The method can effectively improve the yield and safety of the compound shown in the formula (I). Please see the formula in the description.
Preparing method for 1,1-cyclopropyl dimethyl carbinol
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Paragraph 0039; 0044; 0047; 0050; 0053, (2017/08/28)
The invention belongs to the technical field of drug synthesis and relates to a preparing method for 1,1-cyclopropyl dimethyl carbinol. Specifically, the preparing method for the 1,1-cyclopropyl dimethyl carbinol includes the following steps that firstly, under the participation of a catalyst A, a solvent A and an acid-binding agent, diethyl malonate and 1,2-dichloroethane are used for preparing 1,1-cyclopropyl dioctyl phthalate diethyl ester; and secondly, under the participation of a solvent B and a catalyst B, a reducing agent is used for reducing the 1,1-cyclopropyl dioctyl phthalate diethyl ester, and the target product 1,1-cyclopropyl dimethyl carbinol is obtained. Raw materials adopted in the preparing method are cheap, easy to obtain and free of toxins, the activity of the catalysts are high, the solvents can be recycled, and the cost is obviously reduced; and reaction conditions are moderate, the products are easy to separate, the three industrial wastes are little, and the environment-friendly chemical requirement is met. In addition, according to the preparing method, the yield of the target product can be obviously increased, and the total recovery can reach 88% through the two steps.
PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 50; 51, (2016/09/26)
The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
THIENOPYRAZINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 40, (2016/09/26)
The present invention relates to thienopyrazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
