- Preparation method of dioxane-quinazoline derivative
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The invention relates to a preparation method of a dioxane-quinazoline derivative and belongs to the field of medicine intermediate synthesis. Compared with a reported route, the route has the advantages that the procedures are much simpler and the overall yield is increased. An R group includes methyl, ethyl, propyl, isopropyl, methoxyethyl, methoxypropyl, N, N-dimethylaminopropyl, 3-pyrrolidinepropyl, tetrahydropyranyl, cyclopentanyl, 3-piperidine propyl and 3-morpholine propyl, wherein specific information is shown in the description.
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Paragraph 0040-0044
(2019/06/12)
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- Biomimetic synthesis of the calcineurin phosphatase inhibitor dibefurin
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Dibefurin is a Ci-symmetric natural product that acts as an inhibitor of calcineurin phosphatase. A six-step synthesis of this compound is reported, which features an oxidative dimerization of the aromatic polyketide epicoccine as the key step. Dibefurin is proposed to be related to epicolactone, a complex yet racemic fungal metabolite that has recently been discovered. Attempts to access epicolactone from epicoccine and epicoccone B resulted in an unusual dimer that is formed through a hetero-Diels-Alder reaction of a para-quinone methide with an ortho-quinone.
- Ellerbrock, Pascal,Armanino, Nicolas,Trauner, Dirk
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supporting information
p. 13414 - 13418
(2015/02/05)
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- Process development of the PDE4 inhibitor K-34
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A short and practical synthesis of the PDE4 inhibitor K-34 (1) was developed. This synthesis was achieved in four steps and with a 58% overall yield. The unique spiro acetal was created with exceptionally high yield by utilizing the neighbor carboxylic acid assistance. This synthesis also features efficient ketone construction with 4-pyridinylmethyl anion 9 and ester 18, in which overreaction should be prohibited by quick in situ enolate formation. The overall synthesis was carried out under mild conditions and used a simple procedure suitable for large-scale production.
- Yanagisawa, Arata,Taga, Masashi,Atsumi, Toshiyuki,Nishimura, Koichiro,Ando, Kyoji,Taguchi, Tsuyoshi,Tsumuki, Hiroshi,Chujo, Iwao,Mohri, Shin-Ichiro
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experimental part
p. 376 - 381
(2012/02/01)
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- PROCESS FOR PREPARATION OF 1,3-BENZODIOXOLE-2-SPIRO- CYCLOALKANE DERIVATIVES
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(wherein R1 represents hydroxy or substituted or unsubstituted lower alkoxy; R2 represents an aromatic heterocyclic group or the like; Y represents lower alkyl or the like; and n represents an integer of from 1 to 6)For example, a process for preparing a 1,3-benzodioxole-2-spirocycloalkane derivative represented by the above formula (VII), which comprises adding a base to a mixture containing a compound represented by the above formula (V) and a compound represented by the above formula (VI); and allowing the compound represented by the above formula (V) to react with the compound represented by the above formula (VI), are provided.
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Page/Page column 16
(2008/06/13)
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- SELECTIVE DEMETHYLATIONS IN 2,3,4-TRIMETHOXYARYL CARBONYL COMPOUNDS
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2,3,4-Trimethoxybenzaldehyde, -acetophenone and -benzoic acid give the corresponding 2,3-dihydroxy-4-methoxy compounds in good yield on treatment with BCl3.
- Kaisalo, Leena,Latvala, Anita,Hase, Tapio
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p. 645 - 648
(2007/10/02)
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