38 results about "Group transformation" patented technology

The novel intermediate compound which can be efficiently utilized in the synthesis of carotenoid compounds based on the sulfone chemistry, the preparation method of the same, and the practical synthetic process for preparing β-carotene by the use of the above novel compound are disclosed. The synthesis of β-carotene is characterized by the double elimination reactions of the C40 compound containing both the benzenesulfonyl group and the group X (either halogen or ether), which can be prepared by the coupling reaction of the novel C10 dialdehyde with two equivalents of the C15 allylic sulfone, followed by the functional group transformation of the resulting C40 diol either to the corresponding halide or to the ether, to produce the fully conjugated polyene chain.

The invention relates to a fully-substituted 3-nitroindole compound as well as a preparation method and application of the fully-substituted 3-nitroindole compound and belongs to the technical field of pharmaceutical chemistry. The compound has a structure shown as a formula (I): the formula (I) is shown in the description; an intermediate has a general structure shown as a formula (II): the formula (II) is shown in the description. A synthesis method of the fully-substituted 3-nitroindole compound and the intermediate of the fully-substituted 3-nitroindole compound, disclosed by the invention, has the characteristics of easiness of obtaining raw materials, moderate reaction conditions, short reaction steps, high yield, low synthetic cost and the like, and is especially suitable for industrial production. The structure of the fully-substituted 3-nitroindole compound has a plurality of fluorine atoms; the fluorine element is introduced so that the bioactivity of the compound is doubled; meanwhile, nitro of the compound is easily subjected to functional group transformation and a foundation is laid for further result modification. The fully-substituted 3-nitroindole compound has various potential pharmaceutical activities. The anti-tumor activity of the fully-substituted 3-nitroindole compound is primarily researched. A research shows that one part of the compound has certain anti-tumor activity and has a wide application prospect.

The novel C dialdehyde compound which can be efficiently utilized in the synthesis of carotenoid compounds based on the sulfone chemistry, the preparation method of the same, and the expeditious and practical synthetic processes for lycopene and β-carotene by the use of the above novel compound are disclosed. The syntheses of lycopene and β-carotene are characterized by the processes of the coupling reaction between two equivalents of geranyl sulfone or cyclic geranyl sulfone and the above C dialdehyde, the functional group transformation reactions of the diol in the resulting C 40 coupling products to X's (either halogens or ethers), and the double elimination reactions of the functional groups of the benzenesulfonyl and X to produce the fully conjugated polyene chain of the carotenoids.

The invention provides a Gaussian N75 printable wide and narrow newspaper transformation method. Through the steps of triangular plate cutting, base platform hole expansion, moving quantity modification and main paper leading roller group transformation, the narrow-width newspaper printing requirements with great dimension differences can be further met on the basis of maintaining the original wide-width newspaper printing, in addition, the cost of the transformation method is low, and in addition, the wasted work hours are few. In addition, the invention simultaneously provides a printable wide and narrow newspaper double-width rotary press, which is different from ordinary products, through adopting a novel triangular plate structure, a main paper leading roller structure, a transmission structure and a design of sufficient triangular plate horizontal moving quantity, the fast regulation can be realized, so the narrow-width newspaper printing requirements with great dimension differences can be met.

The invention discloses a laboratory-scale synthesizing and curing method of a terminal carboxyl liquid fluorine elastomer. The method comprises the following steps: dissolving a fluorine elastomer in an organic solvent; carrying out oxidative degradation reaction in the presence of oxidant and alkali, in which the reaction time lasts for 8-24 hours, and the reaction temperature changes in a range of 10-40 DEG C; and controlling the dripping speed of the oxidant and the alkali via a peristaltic pump to obtain the terminal carboxyl liquid fluorine elastomer. The synthesizing method has the characteristics of few by-products, simplicity and controllability, and high yield. The terminal carboxyl liquid fluorine elastomer can be cured by reacting with carbodiimide-containing compounds under the normal temperature; the cured product has the characteristics of high mechanical performance, high resistance to high temperature and low temperature and high resistance to chemical media; the terminal carboxyl liquid fluorine elastomer can be used for preparing sealants and adhesives with resistance to chemical media and can also be used for preparing terminal-sealed liquid fluorine elastomers such as hydroxyl, silane, epoxy and amino and the like through terminal group transformation reaction.

The invention relates to a method of using the close-ring reaction of cyclopropane which is induced by the thermal rearrangement of methylene cyclopropyl aldehyde and hydrazide or hydrazine hydrate after the open-ring for synthesizing 2, 3-dibasic pyrrole amine derivatives. No matter substituents in substrates of the methylene cyclopropane aldehyde are aromatic rings with various withdrawing electron or donating electron groups or various alkyls and hydrogen for the substitution of various functional groups in the reaction, the reaction can be carried out successfully. And corresponding pyrrole amine derivatives can be obtained at the yield from medium to perfect. In the reaction, the substrates with pyrrole amine skeletons are generated and are proved to be provided with various perfect biological activities and pharmacological activities in previous researches. Simultaneously, the compounds have perfect modification characteristics. Especially in the synthesis of the pyrrole amine compounds without any protecting group, free amino groups with potential application value can realize various functional-group transformations conveniently. No catalysts and additives are required to be added in the reaction. Therefore, the method is environment-friendly, and products can be purified easily. The reaction can well satisfy the requirement of preparing compounds with high purity in medical chemistry.

The invention discloses a construction method of a multi-dimensional similar-orthogonal pseudo-random extended matrix, which comprises the steps of screening and combining primitive polynomials of f1(x), f2(x), ..., fn(x), then carrying out group transformation and numerical conversion, constructing a similar-orthogonal pseudo-random matrix M, then passing through a comb filter with the thresholdof sigma 1, selecting a code group with good relevance and constructing a matrix PN; and then selecting another group of f1'(x), f2'(x), ..., fn'(x), screening, combining, carrying out the group transformation for obtaining a matrix M', then passing through the comb filter with the threshold of sigma 2 which is equal to 0, selecting the completely orthogonal code group, constructing a PN' matrix,finally carrying out direct product operation on the previously produced PN matrix and the completely orthogonal PN' matrix, and obtaining an MSPE matrix PN-PN' after extension. The MSPE matrix PN-PN' after extension through the method has the orthogonal property which is similar to the Walsh matrix, when the MSPE matrix PN-PN' after extension is applied in a CDMA system, the MSPE matrix PN-PN' can obtain the effects which are similar to those of the Walsh matrix. Meanwhile, the size of the matrix is different with the Walsh matrix which is limited by the order of 2, and can be arbitrary value.

The novel C dialdehyde compound which can be efficiently utilized in the synthesis of carotenoid compounds based on the sulfone chemistry, the preparation method of the same, and the expeditious and practical synthetic processes for lycopene and β-carotene by the use of the above novel compound are disclosed. The syntheses of lycopene and β-carotene are characterized by the processes of the coupling reaction between two equivalents of geranyl sulfone or cyclic geranyl sulfone and the above C dialdehyde, the functional group transformation reactions of the diol in the resulting C 40 coupling products to X's (either halogens or ethers), and the double elimination reactions of the functional groups of the benzenesulfonyl and X to produce the fully conjugated polyene chain of the carotenoids.

The invention discloses a novel method for preparing 4-(3-chlorine-4-fluorophenylamino)-7-methoxyl-6-(3-morpholinepropoxy)quinazoline (gefitinib, I). The method comprises the following steps of: preparing an intermediate (VI), performing functional group transformation twice under a hydrogenation condition to generate 2-(N,N-dimethylformylimido)-4-methoxyl-5-(3-morpholinepropoxy)cyanophenyl (VIII), and performing ring closure rearrangement on the obtained (VIII) and 3-chlorine-4-fluoroaniline to generate the gefitinib (I). The method is short in steps and high in yield in each step, the intermediate is convenient to purify, a target product has high purity, and the method is suitable for industrial production.

The invention discloses an asymmetric full-synthesis method of a natural product (+)-Tanikolide, belonging to the field of organic synthesis. The (+)-Tanikolide has a structure as shown in the specification; and chiral tertiary alcohol is created through a synthesis strategy which is completely different from that of the existing document, and the synthesis of (+)-Tanikolide is correspondingly selectively finished. The synthesis path takes the optically active amino alcohol as a raw material and comprises the following steps of: performing an oxidation reaction to obtain amino aldehyde with maintained configuration; creating chiral quaternary carbon through three-step continuous reaction including Witting reaction, [2,3]-Meisenheimer rearrangement and catalytic hydrogenation; and finally performing functional group transformation to obtain a target product. The total yield is 35%. The operation is convenient, the reaction conditions are moderate, the method is suitable for large-scale preparation, and the optical rotation of the synthesis product is consistent with the optical rotation and optical rotation direction of the natural product (+)-Tanikolide.