在甲醇中进行光解时,二叔丁基次膦叠氮化物(4; R = Bu t)在失去氮的情况下重排,得到NP NP-二叔丁基膦酰胺酸甲酯(6; R = Bu t,X = OMe)(71%),大概是通过被溶剂捕获的单体偏亚膦酸酯(5; R = Bu t)。尽管二叔丁基次膦酰胺在乙醇中也是主要产物,而在异丙醇中是主要产物,但在其他醇和叔丁胺中也会发生类似的重排。二isopropylphosphinic叠氮化物(4; R = PR我)以类似的方式的行为,但在甲醇中较少受阻二乙基次膦叠氮化物(4; R = ET)患有广泛溶剂分解,以二乙基次膦酸甲酯。
There is described a process for preparing an enamine of formula (IX): ##STR1## where R.sup.2 is a carboxylic acid protecting group and R.sup.3 is the residue of a carboxylic acid derived acyl group and where R.sup.5 and R.sup.6 are the same or different C.sub.1-4 alkyl or C.sub.7-10 aralkyl groups; or taken together with the adjacent nitrogen atom form a heterocyclic ring containing from 4 to 8 carbon atoms and optionally a further heteroatom selected from oxygen and nitrogen; by reacting a compound of formula (XII): ##STR2## with an amine of formula HNR.sup.5 R.sup.6, the reactant of formula (XII) being prepared by reaction of an appropriate enol derivative with a phosphorus reagent. The enamines of formula (IX) are useful in the preparation of 3-hydroxycephalosporins.
Process for producing 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine
申请人:Toyama Chemical Co., Ltd.
公开号:US04704459A1
公开(公告)日:1987-11-03
This invention relates to a process for industrially producing a 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine derivative and a salt thereof which are useful as an antibacterial agent, and also to intermediates therefor and processes for producing the intermediates.
Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors
作者:Andreas Ritzén、Morten D. Sørensen、Kevin N. Dack、Daniel R. Greve、Anders Jerre、Martin A. Carnerup、Klaus A. Rytved、Jesper Bagger-Bahnsen
DOI:10.1021/acsmedchemlett.6b00087
日期:2016.6.9
Janus kinase (JAK) inhibitors are emerging as novel and efficacious drugs for treating psoriasis and other inflammatory skin disorders, but their full potential is hampered by systemic side effects. To overcome this limitation, we set out to discover soft drug JAK inhibitors for topical use. A fragment screen yielded an indazole hit that was elaborated into a potent JAK inhibitor using structure-based
A compound of the Formula I
1
a prodrug thereof, or the pharmaceutically acceptable salt of the compound or prodrug; wherein X, Y, a, b, c, d, R
1
, R
2
, R
3
, R
4
, R
5
, R
6
and R
7
are as defined above and are useful to treat inflammation and other immune disorders. The present invention also relates to pharmaceutical compositions that include compounds of Formula I and a pharmaceutically acceptable carrier. Moreover, the present invention relates to methods of using the above-described compounds and compositions to treat and prevent diseases and conditions.