C07D317/22

INTERMEDIATE OF ERIBULIN AND SYNTHESIS METHOD AND USE THEREOF
20220204523 · 2022-06-30 ·

An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.

PROCESSES AND INTERMEDIATES FOR PREPARING MCL1 INHIBITORS

The present disclosure relates to methods and intermediates for the synthesis of certain compounds that inhibit MCL1, for use in the treatment of cancers.

METHOD FOR PREPARING GLUCOPYRANOSYL DERIVATIVES AND INTERMEDIATES THEREOF

A method for preparing glucopyranosyl derivatives as sodium dependent glucose cotransporter (SGLT) inhibitors, an intermediate thereof, and a method for preparing the intermediate.

METHOD FOR PREPARING GLUCOPYRANOSYL DERIVATIVES AND INTERMEDIATES THEREOF

A method for preparing glucopyranosyl derivatives as sodium dependent glucose cotransporter (SGLT) inhibitors, an intermediate thereof, and a method for preparing the intermediate.

KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF
20220411365 · 2022-12-29 ·

Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.

Ketamine derivatives and compositions thereof

Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.

Azole analogues and methods of use thereof
11390613 · 2022-07-19 · ·

Disclosed herein are analogues of itraconazole that are both angiogenesis and hedgehog signaling pathway inhibitors, formulations thereof, including liposome formulations thereof. The compounds are expected to be useful in the treatment of cell proliferation disorders such as cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.

Composition and method for manufacturing device using same
11142495 · 2021-10-12 · ·

An onium salt and a composition having high sensitivity and excellent pattern characteristics such as LWR, which is preferably used for a resist composition for a lithography process using two active energy rays of a first active energy ray such as an electron beam or an extreme ultraviolet and a second active energy ray such as UV.

METHOD FOR PRODUCING FLUOROVINYL ETHER COMPOUND

An object of the present invention is to provide, for example, a novel method for synthesizing a fluorovinyl ether compound from a fluorine-containing vinyl compound. This problem is solved by a method for producing a compound represented by formula (1):

##STR00001##

wherein
R.sup.a1 is a hydrogen atom, a halogeno group, an alkyl group, a fluoroalkyl group, or an aromatic group optionally having one or more substituents,
Rf is a fluoro group or a perfluoroalkyl group,
R.sup.a2 is a hydrogen atom, a halogeno group, an alkyl group, a fluoroalkyl group, or an aromatic group optionally having one or more substituents, or
(i) R.sup.a1 and R.sup.a2, (ii) R.sup.a1 and Rf, or (iii) Rf and R.sup.a2 may be linked to each other,
R.sup.b1 is R.sup.S,
R.sup.b2 is a hydrogen atom or R.sup.S,
R.sup.b3 is a hydrogen atom or R.sup.S, or
two or three of R.sup.b1, R.sup.b2, and R.sup.b3, taken together with the adjacent carbon atom, may form a ring optionally having one or more substituents, and
R.sup.S, in each occurrence, is the same or different and represents a hydrocarbon group optionally having one or more substituents, the method comprising
step A of reacting a compound represented by formula (2):

##STR00002##

wherein
R.sup.x is a leaving group, and
other symbols are as defined above,
with a compound represented by formula (3):

##STR00003##

wherein the symbols in the formula are as defined above, in the presence of a transition metal catalyst.

KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF

Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.